| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg | |||
| 25mg | |||
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| Other Sizes |
| Targets |
PhTx-74 diHCl targets AMPA receptors (AMPARs), specifically the GluR3 and GluR1 subunits. AMPA receptors are ionotropic glutamate receptors that mediate fast excitatory neurotransmission in the central nervous system. PhTx-74 diHCl inhibits GluR3 with an IC50 of 263 nM and GluR1 with an IC50 of 296 nM. It also inhibits GluR5. Its activity has been characterized in electrophysiological studies.
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| ln Vitro |
When oocytes coexpressed γ-2 with the two primary isoforms of GluA2R-containing AMPARs (GluA1/A2R and GluA2R/A3), philanthotoxin 74 exhibited selective inhibition in the micromolar dose range. At 500 μM, philanthotoxin 74 has been shown to totally inhibit GluA1/A2R receptors while just slightly inhibiting GluA2R/A3 receptors (10%). When tested at 100 and 500 μM concentrations, philanthotoxin 74 demonstrated negligible channel blocking of GluA2R/A3, but significant channel blocking of GluA1/A2R (greater than 80%). When evaluated at the highest dose of 300 μM, oocytes expressing GluA2R alone or homopolymeric GluA2R showed less than 5% inhibition, making them essentially inert to Zanthoxylin 74 in the concentration range of 0.1-300 μM. With an IC50 value of roughly 30 μM, philanthotoxin 74 non-selectively inhibits these receptors both in the presence and absence of gamma-2 [1].
PhTx-74 diHCl demonstrates potent inhibition of AMPA receptors in vitro. It inhibits GluR3 and GluR1 with IC50 values of 263 and 296 nM, respectively. At micromolar concentrations, it inhibits AMPARs containing GluA2R, specifically GluA1/A2R and GluA2R/A3, when co-expressed with γ-2 in oocytes. Its activity is assessed by electrophysiological recordings (two-electrode voltage clamp) in Xenopus oocytes expressing recombinant AMPA receptor subunits. |
| ln Vivo |
In vivo effects of PhTx-74 diHCl have been studied in animal models. As an AMPA receptor antagonist, it modulates glutamatergic neurotransmission, which has implications for neurological and psychiatric disorders. Its ability to cross the blood-brain barrier and its in vivo efficacy have been demonstrated in preclinical studies. Detailed in vivo efficacy data are available in the literature.
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| Enzyme Assay |
AMPA receptor inhibition assays are performed using Xenopus oocytes expressing recombinant AMPA receptor subunits (GluR1, GluR3, GluA1/A2R, GluA2R/A3). Two-electrode voltage clamp electrophysiology is used to record glutamate-induced currents. Oocytes are injected with cRNA for the receptor subunits and γ-2 accessory protein. PhTx-74 diHCl is applied at varying concentrations, and inhibition of glutamate-induced currents is measured. IC50 values are determined by non-linear regression analysis. Each concentration is tested in multiple oocytes.
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| Cell Assay |
Cellular AMPA receptor inhibition is evaluated in neuronal cell lines or primary neuronal cultures. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with PhTx-74 diHCl at various concentrations (0.1-100 µM). AMPA-induced calcium influx is measured using fluorescent calcium indicators (Fura-2, Fluo-4). Alternatively, patch-clamp electrophysiology is used to record AMPA-induced currents. Cell viability is assessed using MTT or LDH assays. Each experiment includes known AMPA receptor antagonists (e.g., CNQX, NBQX) as positive controls.
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| Animal Protocol |
In vivo studies are conducted in rodent models of neurological disorders involving glutamatergic dysfunction. PhTx-74 diHCl is administered via intracerebroventricular (ICV) injection or systemic administration. Behavioral assessments may include tests of learning and memory, motor function, and pain sensitivity. Brain tissue is collected for neurochemical analysis and histology. Sample sizes typically range from 8-12 animals per group. Detailed protocols are available in the literature.
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| ADME/Pharmacokinetics |
PhTx-74 diHCl has a molecular weight of 507.54 g/mol and a molecular formula of C24H44Cl2N4O3. Chemical name: (S)-N-(1-((7-((4-aminobutyl)amino)heptyl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)butyramide dihydrochloride. Purity: ≥98%. Solubility: DMSO: 100 mM; Water: 100 mM. Storage: typically at -20°C. Appearance: solid.
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| Toxicity/Toxicokinetics |
Limited toxicology data are available for PhTx-74 diHCl as it is a research compound. As an AMPA receptor antagonist, potential toxicities may include effects on glutamatergic neurotransmission. Standard toxicology studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on the central nervous system. No clinical trials have been reported for this compound.
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| References | |
| Additional Infomation |
Philanthotoxin 74 is a tyrosine derivative.
PhTx-74 diHCl is also known as Philanthotoxin 74 dihydrochloride, PhTx 74 dihydrochloride, and Philanthotoxin 74 hydrochloride. It is a synthetic analog of the naturally occurring wasp venom toxin philanthotoxin-4,3,3. It is an AMPAR antagonist that inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively. No clinical trials or regulatory approvals have been reported. The compound is for research use only. |
| Molecular Formula |
C24H44CL2N4O3
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|---|---|
| Molecular Weight |
507.54
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| Exact Mass |
506.279
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| Elemental Analysis |
C, 56.80; H, 8.74; Cl, 13.97; N, 11.04; O, 9.46
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| CAS # |
1227301-51-0
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| Related CAS # |
401601-11-4;1227301-51-0 (HCl);
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| PubChem CID |
46213501
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
33
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| Complexity |
468
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C(NCCCCCCCNCCCCN)[C@@H](NC(CCC)=O)CC1=CC=C(O)C=C1.[H]Cl.[H]Cl
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| InChi Key |
HWTJQQMIKVJWLH-IKXQUJFKSA-N
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| InChi Code |
InChI=1S/C24H42N4O3.2ClH/c1-2-10-23(30)28-22(19-20-11-13-21(29)14-12-20)24(31)27-18-8-5-3-4-7-16-26-17-9-6-15-25/h11-14,22,26,29H,2-10,15-19,25H2,1H3,(H,27,31)(H,28,30)2*1H/t22-/m0../s1
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| Chemical Name |
(S)-N-(1-((7-((4-aminobutyl)amino)heptyl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)butyramide dihydrochloride
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| Synonyms |
PhTx 74PhTx74 Philanthotoxin 74 Philanthotoxin74 Philanthotoxin-74 HCl
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~100 mg/mL (~197.03 mM)
H2O : ~50 mg/mL (~98.51 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (98.51 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9703 mL | 9.8514 mL | 19.7029 mL | |
| 5 mM | 0.3941 mL | 1.9703 mL | 3.9406 mL | |
| 10 mM | 0.1970 mL | 0.9851 mL | 1.9703 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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