Prostate-specific membrane antigen (PSMA). No IC50, Ki, EC50, or binding affinity values are provided in these manuscripts. [1][2]
The target of [¹⁸F]PSMA-1007 is prostate-specific membrane antigen (Glutamate Carboxypeptidase 2, GCPII/PSMA). PSMA is a type II transmembrane glycoprotein with limited expression in normal prostate epithelial cells but is significantly overexpressed in prostate cancer cells, with expression levels rising with increasing tumor dedifferentiation and hormone resistance. Following intravenous injection, the PSMA-1007 ligand moiety of [¹⁸F]PSMA-1007 specifically binds to PSMA-positive tumor cells, and the positrons emitted by the radioisotope fluorine-18 enable non-invasive visualization of PSMA-expressing tumors via PET/CT or PET/MRI imaging.

In in vitro PSMA binding affinity assays, the PSMA-1007 ligand exhibits a binding affinity of 6.7 ± 1.7 nM for PSMA. In PSMA-positive LNCaP cells, PSMA-1007 demonstrates an exceptionally high internalization rate (67% ± 13%), indicating that the ligand not only binds efficiently to PSMA but is also internalized into cells, making its structure compatible with therapeutic PSMA-617 radioligands. This favorable internalization property is an important basis for its use as a companion diagnostic agent in theranostic approaches.

- Uptake in sympathetic trunk ganglia in patients with biochemical recurrence of prostate cancer ([1]): In 28 patients (median age 69±9 years), [18F]PSMA-1007 was injected intravenously (baseline: 235±18 MBq; follow-up: 232±19 MBq). PET/CT acquisition started 90-120 min post-injection. The highest uptake was found in coeliac ganglia (SUVmax baseline 3.13±0.85, follow-up 3.11±0.93; SUVmean baseline 2.28±0.64, follow-up 2.28±0.66), followed by cervical ganglia (SUVmax baseline 2.73±0.69, follow-up 2.67±0.74; SUVmean baseline 1.62±0.43, follow-up 1.61±0.43), and sacral ganglia (SUVmax baseline 1.67±0.50, follow-up 1.64±0.52; SUVmean baseline 1.15±0.33, follow-up 1.12±0.34). There was no statistically significant difference in SUVmax or SUVmean between baseline and follow-up scans for a given ganglion station (P_SUVmax = 0.372, P_SUVmean = 0.627). [1]
- Biodistribution in subcutaneous prostate cancer xenograft mouse model (LNCaP) ([2]): LNCaP tumor-bearing mice (n=8) received intravenous injection of [18F]PSMA-1007. Dynamic whole-body PET/CT scans were acquired from 0-120 min post-injection. The kidneys showed the highest accumulation without a washout phase. Peak tumor concentration (Cmax) was 2.86±0.24%ID/g at 112.5±1.64 min (Tmax). Urinary bladder showed predominant excretion (AUC 342.31±36.63%ID/g × min). The salivary glands showed substantial off-target accumulation (AUC 286.28±48.67%ID/g × min, T1/2 238.99±82.52 min). [2]
- Repeatability study in xenograft mice ([2]): Two PET/CT scans (Scan 1 and Scan 2) were performed on the same animals (n=8) 2 days apart. For tumor uptake (SUV), the within-subject coefficient of variation (wCV) was 7.57%, repeatability coefficient (RC) was 20.98%, and intraclass correlation coefficient (ICC) was 0.950 (95% CI: 0.775-0.99, P<0.001). No significant difference in kinetic parameters (K1, k2, k3, Ki) was observed between scans (P>0.05). [2]
- Specificity study in xenograft mice ([2]): Mice (n=5) were treated with the PSMA-selective inhibitor 2-(phosphonomethyl)-pentanedioic acid (2-PMPA, 50 mg/kg) prior to [18F]PSMA-1007 injection. 2-PMPA treatment reduced the net influx rate constant Ki by 32% (baseline: 0.026±0.006, inhibition: 0.018±0.005, P=0.0203) and altered k2 (efflux to blood) and k3 (influx to specific binding tissue). The area under the TAC (AUC) was reduced by 37% (P=0.0027). [2]
- Internal radiation dosimetry in xenograft mice ([2]): Voxel-level dosimetry estimated absorbed doses: tumor 78.25±10.08 mGy/MBq, salivary glands 35.93±6.42 mGy/MBq, kidneys 441.50±59.10 mGy/MBq, heart 10.90±0.82 mGy/MBq, lungs 15.83±1.04 mGy/MBq, liver 11.76±0.82 mGy/MBq, intestine 13.19±0.76 mGy/MBq, urinary bladder 54.16±13.37 mGy/MBq. Organ-level dosimetry gave different values for some organs (e.g., urinary bladder: 441.00±83.18 mGy/MBq). The predicted human effective dose was 1.12×10⁻² ± 1.39×10⁻⁴ mSv/MBq based on ICRP adult reference voxel phantoms. [2]

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[¹⁸F]PSMA-1007 demonstrates excellent tumor-targeting performance in vivo. In LNCaP tumor-bearing nude mouse models, the peak tumor uptake concentration reaches 2.8%ID/g (112 minutes post-injection), with a tumor absorbed dose of 0.079 ± 0.010 Gy/MBq. In organ distribution studies in tumor-bearing mice, LNCaP tumors show a specific uptake value of 8.0 ± 2.4 %ID/g. Small-animal PET/CT experiments clearly visualize LNCaP tumors. In clinical studies, a study of 10 patients with high-risk prostate cancer reported that [¹⁸F]PSMA-1007 PET/CT detected 18 of 19 pelvic lymph node metastases, with the smallest detectable lymph node being only 1 mm in diameter. In a Japanese Phase I/IIa study, using both pathology and imaging as the gold standard, [¹⁸F]PSMA-1007 achieved 100% sensitivity and 100% positive predictive value.

The PSMA binding affinity of the PSMA-1007 ligand is determined using radioligand competitive binding assays. The experimental procedure is as follows: PSMA-positive LNCaP cell membrane homogenates or purified recombinant PSMA protein are incubated with fixed concentrations of radiolabeled reference ligands (such as ¹²⁵I-MIP-1072 or ³H-PSMA-617) and increasing concentrations of unlabeled PSMA-1007 (typically ranging from 0.01 nM to 100 μM) in binding buffer at room temperature for 1-2 hours. After incubation, bound and free fractions are separated by rapid filtration through glass fiber filters, and residual radioactivity on the filters is measured using a γ-counter or liquid scintillation counter. IC₅₀ values are calculated by nonlinear regression analysis, and Ki values are derived using the Cheng-Prusoff equation. PSMA-1007 exhibits a Ki value of 6.7 ± 1.7 nM.

Cellular characterization of PSMA-1007 is evaluated via internalization assays using PSMA-positive cell lines. A typical procedure is as follows: PSMA-positive LNCaP cells and PSMA-negative PC-3 cells (as negative control) are seeded in 24-well plates (1-2×10⁵ cells per well) and cultured in RPMI-1640 medium containing 10% FBS at 37°C, 5% CO₂ until adherent. Cells are incubated with radiolabeled [¹⁸F]PSMA-1007 (typically 0.1-1 μCi/well) at 37°C for various time points (e.g., 10, 30, 60, 120, 240 minutes). Following incubation, cells are washed with acidic buffer (0.05 M glycine-HCl, pH 2.8) to remove surface-bound ligand, then lysed with NaOH. Surface-bound and internalized radioactivities are measured separately using a γ-counter. The internalization rate is expressed as the percentage of internalized radioactivity relative to total bound radioactivity. PSMA-1007 exhibits an internalization rate of 67% ± 13%.

- Xenograft mouse model ([2]): Male BALB/c mice (6 weeks old) were inoculated subcutaneously with 1.0×10⁷ LNCaP cells (human prostate carcinoma, PSMA-positive) in 200 μL PBS into the right flank. Tumor size was measured using calipers: (width² × length)/2. Tumor sizes before imaging: 0.689±0.119 cm³ (caliper) and 0.571±0.078 cm³ (PET/CT software). A total of 13 mice were used: 8 for biodistribution/dosimetry/repeatability studies, 5 for the inhibition group. All experimental procedures were approved by the Institutional Animal Care and Use Committee of Seoul National University Bundang Hospital (No. BA-2002-291-021-02). [2]
- PET/CT imaging protocol ([2]): Animals underwent whole-body PET/CT scans using an animal-dedicated PET/CT system (NanoPET/CT, Mediso) with a 10 cm axial and 12 cm transaxial field of view (FOV). PET spatial resolution was 1.2 mm full width at half-maximum at center of FOV. CT scan (semicircular full trajectory, maximum FOV, 480 projections, 50 kVp, 300 ms, 1:4 binning) was performed immediately before PET scan. Dynamic PET/CT scans were acquired from 0-120 min post-injection of [18F]PSMA-1007. For the repeatability study, a second PET/CT scan was performed 2 days after the first scan. For the specificity study, mice were treated with the PSMA inhibitor 2-PMPA (50 mg/kg, 100 μL) before [18F]PSMA-1007 injection. All animals were anesthetized using 2% isoflurane during scans. [2]
- Patient study protocol ([1]): 28 consecutive patients with biochemical recurrence of prostate cancer (median age 69±9 years, range 49-90) underwent [18F]PSMA-1007 PET/CT at baseline and a follow-up examination between August 2018 and August 2021. [18F]PSMA-1007 was injected as an intravenous bolus (baseline: 235±18 MBq; follow-up: 232±19 MBq). PET/CT acquisition was started 90-120 min post-injection on a Siemens Biograph mCT. Scans were acquired in 3D mode; acquisition time per bed position was 3-4 min. Data were corrected for random, dead time, scatter, and attenuation. Iterative reconstruction using ordered-subsets expectation maximization algorithm (4 iterations, 8 subsets) was performed. [1]

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Preclinical in vivo studies of [¹⁸F]PSMA-1007 are performed using subcutaneous LNCaP prostate cancer xenograft mouse models. The experimental procedure is as follows: 1.0 × 10⁷ LNCaP cells (suspended in 200 μL PBS) are inoculated into the right flank of 6-week-old male BALB/c nude mice, and PET/CT imaging is performed when tumor volumes reach approximately 0.5-0.7 cm³. [¹⁸F]PSMA-1007 is administered as a single injection via the tail vein at a dose of 3.7-11.1 MBq, and dynamic (0-120 minutes) and static scans are acquired using a dedicated small-animal PET/CT system. Regions of interest are drawn to determine radioactive uptake in various organs and tumors, expressed as %ID/g. Specific binding studies are performed using pretreatment with the PSMA inhibitor 2-PMPA (2-(phosphonomethyl)-pentanedioic acid), which reduces tumor uptake by 32%. Repeatability studies show a within-subject coefficient of variation of 7.57% for net influx rates.

- Pharmacokinetic parameters in xenograft mice ([2]): For tumor: Tmax 112.5±1.64 min, Cmax 2.86±0.24%ID/g, AUC 260.98±22.99%ID/g × min (accumulated, no washout). For salivary glands: Tmax 9.25±3.36 min, Cmax 3.25±0.39%ID/g, AUC 286.28±48.67%ID/g × min, T1/2 238.99±82.52 min. For heart: Tmax 0.21±0.03 min, Cmax 8.88±0.82%ID/g, AUC 132.12±9.54%ID/g × min, T1/2 0.79±0.12 min. For lungs: Tmax 0.21±0.03 min, Cmax 3.94±0.37%ID/g, AUC 88.42±7.97%ID/g × min, T1/2 0.39±0.15 min. For kidneys: Tmax 108.75±2.63 min, Cmax 26.10±2.32%ID/g, AUC 2483.88±219.37%ID/g × min (accumulated). For liver: Tmax 0.38±0.05 min, Cmax 4.18±0.47%ID/g, AUC 116.15±12.30%ID/g × min, T1/2 0.44±0.21 min. For intestine: Tmax 1.13±0.25 min, Cmax 1.47±0.14%ID/g, AUC 93.35±9.98%ID/g × min, T1/2 222.73±39.93 min. For urinary bladder: Tmax 110.63±4.38 min, Cmax 4.54±0.57%ID/g, AUC 342.31±36.63%ID/g × min (accumulated). The predominant excretion route was urinary bladder (AUC ~4-fold greater than intestine). [2]
- Uptake in human ganglia ([1]): Coeliac ganglia SUVmax 3.13±0.85 (baseline) and 3.11±0.93 (follow-up); SUVmean 2.28±0.64 (baseline) and 2.28±0.66 (follow-up). Cervical ganglia SUVmax 2.73±0.69 (baseline) and 2.67±0.74 (follow-up); SUVmean 1.62±0.43 (baseline) and 1.61±0.43 (follow-up). Sacral ganglia SUVmax 1.67±0.50 (baseline) and 1.64±0.52 (follow-up); SUVmean 1.15±0.33 (baseline) and 1.12±0.34 (follow-up). [1]
- Absorbed doses ([2]): Voxel-level absorbed doses in xenograft mice: tumor 78.25±10.08 mGy/MBq, salivary glands 35.93±6.42 mGy/MBq, kidneys 441.50±59.10 mGy/MBq, heart 10.90±0.82 mGy/MBq, lungs 15.83±1.04 mGy/MBq, liver 11.76±0.82 mGy/MBq, intestine 13.19±0.76 mGy/MBq, urinary bladder 54.16±13.37 mGy/MBq. Predicted human effective dose: 1.12×10⁻² ± 1.39×10⁻⁴ mSv/MBq. [2]

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The pharmacokinetic profile of [¹⁸F]PSMA-1007 has been characterized in humans and animal models. In healthy volunteers, following a single intravenous injection of 3.7 MBq/kg [¹⁸F]PSMA-1007, the mean blood radioactivity concentration peaks at 5 minutes (47.87 ± 1.05 %ID/mL) and declines to 1.60 ± 0.78 %ID/mL at 6 hours; whole-body radioactivity peaks at 5 minutes (211.05 ± 6.77 × 10³ %ID) and declines to 7.18 ± 3.91 × 10³ %ID at 6 hours. The tracer is primarily excreted via the hepatobiliary pathway with negligible urinary clearance, resulting in low bladder radioactivity that facilitates evaluation of the primary prostate tumor and pelvic lymph nodes. The effective dose of the radiopharmaceutical is approximately 4.4-5.5 mSv per examination (200-250 MBq injection dose). In LNCaP tumor-bearing mouse models, the peak tumor uptake is observed at 112 minutes post-injection (2.8%ID/g).

The studies note that the salivary gland is a dose-limiting organ in PSMA-targeted radionuclide therapy, and the absorbed dose to salivary glands was estimated at 35.93±6.42 mGy/MBq (voxel-level). Procedures were carried out in accordance with ethical standards, with no mention of adverse events in patients or animals. [1][2]

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As a diagnostic radiopharmaceutical, the toxicity of [¹⁸F]PSMA-1007 primarily involves two aspects: the chemical toxicity of the drug itself and radiation exposure risk. In Phase I/IIa clinical trials involving healthy volunteers and prostate cancer patients, all subjects tolerated [¹⁸F]PSMA-1007 well, and no serious adverse events or drug-related adverse reactions were observed. The summary report on marketing authorization also confirms that no undesirable effects associated with [¹⁸F]PSMA-1007 in clinical use have been reported to date. The drug contributes to patients' long-term cumulative radiation exposure, which is associated with an increased risk of cancer. Contraindications include hypersensitivity to the active substance or any of the excipients. Additionally, case reports indicate that [¹⁸F]PSMA-1007 may show false-positive uptake in benign ganglia and lipomas, highlighting the need for careful interpretation.

[1]. PSMA-1007 Uptake in Ganglia of the Sympathetic Trunk and Its Intra-individual Reproducibility. Mol Imaging Biol. 2023 Jun;25(3):554-559.

[2]. Preclinical Evaluation of a Companion Diagnostic Radiopharmaceutical, [18F]PSMA-1007, in a Subcutaneous Prostate Cancer Xenograft Mouse Model. Mol Pharm. 2023 Feb 6;20(2):1050-1060.

- Chemical structure: (3S,10S,14S)-1-(4-((S)-4-carboxy-2-((S)-4-carboxy-2-(6-18F-fluoronicotinamide)butanamido)butanamido)methyl)phenyl)-3-(naphthalen-2-ylmethyl)-1,4,12-trioxo-2,5,11,13-tetraazahexadecane-10,14,16-tricarboxylic acid. [2]
- Radiosynthesis: [18F]PSMA-1007 was produced using a commercial sCUBE radiosynthesizer. The labeling reaction was carried out at 100°C, with radiochemical conversion >88% (by radio-TLC). Purification by HPLC (30% acetonitrile/water for injection in 0.1% trifluoroacetic acid, isocratic), followed by solid-phase extraction (tC18 cartridge). Final formulation in 10% ethanol/0.9% saline. Overall synthesis time ~55 min (including HPLC purification). Isolated radiochemical yield (non-decay-corrected): 30-32% (n=25). Quality control criteria included appearance, identity, radiochemical purity, radionuclidic purity, chemical purity, pH, endotoxins, filter integrity, and sterility. [2]
- Dosimetry methodology ([2]): Both organ-level (MIRD schema) and voxel-level (Monte Carlo simulation using GATE ver 9.0) dosimetry methods were applied. The voxel-level method accounted for tissue heterogeneity and subject-specific variation in activity distribution using PET/CT imaging. [2]
- Clinical relevance ([1]): Physiological [18F]PSMA-1007 uptake in sympathetic trunk ganglia (coeliac, cervical, sacral) can be misinterpreted as PSMA-positive lymph node metastases. The study provides SUVmax and SUVmean values and demonstrates good intra-individual reproducibility of uptake in follow-up scans, which may help differentiate ganglia from malignant lesions. The cervical and coeliac ganglia were found along the vertebra in the area of T1/T2 and T12/L1, respectively; sacral ganglia were localized in the presacral region. In most cases, ganglia could be identified pairwise. [1]
- Theranostic application ([2]): [18F]PSMA-1007 shares a similar motif with [177Lu]Lu-PSMA-617 and can be used as a surrogate imaging radiopharmaceutical for PSMA-targeted radionuclide therapy. The study demonstrates the potential for voxel-level dosimetry to guide personalized therapy and minimize off-target toxicity (e.g., xerostomia, salivary gland hypofunction, renal toxicity). [2]

C54H64F3N9O18

1184.1306848526

1030.37

C, 57.08; H, 5.38; F, 1.84; N, 10.87; O, 24.83

2226894-58-0

2093321-19-6

153327302

White to off-white solid powder

12

22

31

84

2140

5

C[N+](C)(C)C1=NC=C(C=C1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)NCC2=CC=C(C=C2)C(=O)N[C@@H](CC3=CC4=CC=CC=C4C=C3)C(=O)NCCCC[C@@H](C(=O)O)NC(=O)N[C@@H](CCC(=O)O)C(=O)O.C(=O)(C(F)(F)F)[O-]

QQFSTGSNRLIZGD-ACXPFIKISA-N

InChI=1S/C52H63N9O16.C2HF3O2/c1-61(2,3)41-21-17-35(29-54-41)46(69)56-37(19-23-43(64)65)49(72)57-36(18-22-42(62)63)47(70)55-28-30-11-15-33(16-12-30)45(68)58-40(27-31-13-14-32-8-4-5-9-34(32)26-31)48(71)53-25-7-6-10-38(50(73)74)59-52(77)60-39(51(75)76)20-24-44(66)67;3-2(4,5)1(6)7/h4-5,8-9,11-17,21,26,29,36-40H,6-7,10,18-20,22-25,27-28H2,1-3H3,(H11-,53,55,56,57,58,59,60,62,63,64,65,66,67,68,69,70,71,72,73,74,75,76,77);(H,6,7)/t36-,37-,38-,39-,40-;/m0./s1

[5-[[(2S)-4-carboxy-1-[[(2S)-4-carboxy-1-[[4-[[(2S)-1-[[(5S)-5-carboxy-5-[[(1S)-1,3-dicarboxypropyl]carbamoylamino]pentyl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]carbamoyl]phenyl]methylamino]-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]carbamoyl]-2-pyridinyl]-trimethylazanium;2,2,2-trifluoroacetate

PSMA-1007; PSMA1007; 2226894-58-0; orb1785986; PSMA 1007;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: ~125 mg/mL (105.6 mM)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)