| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Cryptocine (2.5–7.5 μM; 24 h) induces mitochondrial exhaustion in A375 and Hs294t melanoma cells in a concentration-dependent manner and activates the AMPKα1/2-LKB1 pathway [1]. Cryptocine (2.5–10 μM) inhibits LPS-induced nitric oxide production in RAW 264.7 cells and exerts anti-inflammatory effects by inhibiting DNA binding activity during NF-κB activation [4]. Cryptocine (0.5–2 μM; 24 h) inhibits the levels of p-STAT3 and IL-23 in human hepatocellular carcinoma HepG2 cells treated with 200 ng/mL IL-6 for 24 h in a dose-dependent manner [6]. Cryptocine (1–20 μM; hypoxic conditions; 24 h) reduced hypoxia-induced HIF-1α protein levels in T47D, 4T1, MCF-7, and MDA-MB-231 breast cancer cells in a time- and dose-dependent manner [8]. Cryptocine (0–100 μg/mL; 72 h) extracted from Cryptolopis sanguinolenta was cytotoxic to the Jurkat leukemia cell line with a CC50 value <62.56 μg/mL [9]. Cryptocine (10 μM–1.69 × 10⁻⁴ μM; 48 h) inhibited the activity of late IV/V stage gametophytes of Plasmodium falciparum (NF54) with an IC50 value of 1965 nM [12]. Cryptolepine (0.5-1.2 μM; 48 h) effectively inhibited the migration of unstimulated and WNT3a-stimulated DLD1 colorectal cancer cells, with IC30 (0.5 μM) and IC50 concentrations of [14].
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| ln Vivo |
Cryptocline (10 mg/kg; intraperitoneal injection; three times a week for 24 days) inhibited the growth of melanoma in athymic nude mice by interfering with mitochondrial dynamics and biosynthesis, resulting in a 68% reduction in tumor volume and a 61% reduction in tumor weight[1]. Cryptocline (7.0–112.6 mg/kg/d; subcutaneous injection; once daily for 4 days) did not significantly reduce parasitemia levels of Plasmodium berghei in mice[3]. Cryptocline (10–40 mg/kg; intraperitoneal or oral injection; once daily for 4 days) showed dose-dependent anti-inflammatory activity in an acute inflammatory rat model without causing gastric damage[4]. Cryptocine (10-40 mg/kg; intraperitoneal injection) showed dose-dependent anti-inflammatory activity in a carrageenan-induced rat paw edema model, such as inhibiting lipopolysaccharide (LPS)-induced microvascular permeability; cryptocine (10-40 mg/kg; intraperitoneal injection) also showed dose-dependent analgesic activity in an acetic acid-induced mouse writhing model [7]. Cryptocine (5-20 mg/kg; intraperitoneal injection; once every 2 days; for a total of 7 doses) dose-dependently inhibited the growth of 4T1 tumors in BALB/c mice, with a tumor growth inhibition rate (TGI) of 71.5% in the 20 mg/kg dose group. Its mechanism of action involves the inhibition of HIF-1-mediated glycolysis and ATP production [8].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: A375, Hs294t Tested Concentrations: 2.5, 5.0, 7.5 μM Incubation Duration: 24 hours Experimental Results: Compared with the vector control group, the protein levels of Mfn1, Mfn2, Opa1, and Drp1 decreased in a concentration-dependent manner. The total mTOR protein and phosphorylated mTOR protein levels, as well as the phosphorylation levels of downstream targets p70S6K and 4E-BP1, decreased in a concentration-dependent manner; the total p70S6K and 4E-BP1 levels were not affected. The protein levels of PGC-1α, SIRT1, Opa1, and c-Myc decreased in a concentration-dependent manner. ELISA detection [6] Cell Types: IL-6 treated human hepatocellular carcinoma HepG2 cells Tested Concentrations: 0.5, 1, 2 μM (in the presence of 200 ng/mL IL-6) Incubation Duration: 24 hours Experimental Results: p-STAT3 and IL-23 levels were inhibited in a dose-dependent manner. When co-treated with 5 μM nicotinamide at a concentration of 0.5 μM, the inhibitory effect on p-STAT3 and IL-23 levels was additive. Western Blot Analysis [8] Cell Types: T47D, 4T1, MCF-7, and MDA-MB-231 breast cancer cells Tested Concentrations: 1-20 μM Incubation Duration: 24 hours under hypoxic conditions Experimental Results: Reduced hypoxia-induced HIF-1α protein levels in T47D, 4T1, MCF-7, and MDA-MB-231 breast cancer cells. Dose-dependently inhibited hypoxia-induced expression of GLUT-1, LDHA, PFKFB3, p-PFKFB3, and PFK-1 proteins. It dose-dependently reduced phosphorylation of Ras, pc-Raf, p-MEK1/2, p-ERK1/2 (MAPK pathway), p-mTOR, p-p70S6K, p-4E-BP1, and p-eIF4E (mTOR pathway and eIF4E phosphorylation); and increased phosphorylation of p-AMPKα and p-TSC2. |
| Animal Protocol |
Animal/Disease Models:Athymic nude mice (female, 4-5 weeks old) [1]
Doses: 10 mg/kg Route of Administration: Intraperitoneal injection; 3 days a week; for 24 days Experimental Results: Tumor volume decreased by 68%; average wet tumor weight decreased by 61%; tumor ATP content decreased by 32%; phosphorylated Drp1, c-Myc, SIRT1 and PGC-1α protein levels decreased; AMPKα1/2 phosphorylation increased; 4E-BP1 phosphorylation decreased. Animal/Disease Models:Swiss albino mice (TO strain, male, average weight 25 g, no endocytic red blood cells, infected with Plasmodium berghei)[3] Doses:7.0, 14.1, 28.2, 56.3, 112.6 mg/kg/d Route of Administration:Subcutaneous injection; once daily; 4 days Experimental Experimental Results:No significant effect on Plasmodium berghei seroprevalence, with average parasitemia values ranging from 33.04% to 46.44%, which was not significantly lower than that of the control group mice. Animal/Disease Models: Wistar rats (male, 120–200 g) carrageenan-induced paw edema model, LPS-induced microvascular permeability model and acetic acid-induced writhing model [7] Doses: 10, 20, 40 mg/kg Route of Administration: Intraperitoneal injection; single administration 1 hour before carrageenan injection Experimental Results: 1. At 3 hours after administration (peak edema period), paw edema was significantly inhibited in a dose-dependent manner. 2. LPS-induced microvascular permeability was significantly inhibited in a dose-dependent manner. 3. Carrageenan-induced pleurisy was inhibited by 23.6%, 35.3% and 51.2% in a dose-dependent manner at doses of 10, 20 and 40 mg/kg, respectively. 4. Writhing response was significantly inhibited in a dose-dependent manner. Animal/Disease Models:BALB/c (female, 4-6 weeks old, 18-22 g, 4T1 tumor xenograft model) [8] Doses: 5, 10, 20 mg/kg Route of Administration: Intraperitoneal injection; once every 2 days; a total of 7 injections Experimental Results: Tumor weight decreased, and tumor growth inhibition rate (TGI) was 45.8% (10 mg/kg) and 71.5% (20 mg/kg), respectively. HIF-1α protein expression in the tumor decreased in a dose-dependent manner; tumor lactate levels decreased by 54.1% (10 mg/kg) and 68.4% (20 mg/kg), respectively. Tumor ATP production decreased in a dose-dependent manner. At doses of 10 and 20 mg/kg, the ratio of phosphorylated eIF4E to total eIF4E in the tumor decreased. |
| References |
| Molecular Formula |
C16H12N2
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|---|---|
| Molecular Weight |
232.29
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| CAS # |
480-26-2
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
N1=C2C=CC=CC2=C3C1=CC=4C=CC=CC4N3C
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3050 mL | 21.5248 mL | 43.0496 mL | |
| 5 mM | 0.8610 mL | 4.3050 mL | 8.6099 mL | |
| 10 mM | 0.4305 mL | 2.1525 mL | 4.3050 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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