| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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GFB-8438 is a novel, highly potent and subtype specific TRPC5 inhibitor with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. It shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.
| ln Vitro |
GFB-8438 (1 μM) pretreatment of mouse podocytes for 30 min, followed by protamine sulfate incubation, substantially prevented synaptopodin loss and cytoskeletal remodeling[1].
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|---|---|
| ln Vivo |
In a hypertensive deoxycorticosterone acetate (DOCA)-salt rat model of focal segmental glomerulosclerosis (FSGS), GFB-8438 (30 mg/kg; sc; daily for 3 weeks) is effective in lowering both total protein and albumin concentrations in urine[1]. Cl, VSS, and t1/2 were 31 mL/min/kg, 1.17 L/kg, and 0.5 hours, respectively, following GFB-8438 (1 mg/kg; IV) treatment[1].
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| Animal Protocol |
Animal/Disease Models: Sprague Dawley rats (DOCA-salt rat model of FSGS)[1]
Doses: 30 mg/kg Route of Administration: sc; daily for 3 weeks Experimental Results: Significant reduction in urine protein concentrations. Animal/Disease Models: 6-8 weeks old male SD rats[1] Doses: 1 mg/kg Route of Administration: iv (pharmacokinetic/PK Analysis) Experimental Results: The Cl, Vss, and t1/2 were 31 mL/min/kg, 1.17 L/kg, and 0.5 hrs (hours), respectively. |
| References |
| Molecular Formula |
C₁₆H₁₄CLF₃N₄O₂
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|---|---|
| Molecular Weight |
386.7562
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| Exact Mass |
386.075
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| CAS # |
2304549-73-1
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| PubChem CID |
138471783
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.52±0.1 g/cm3(Predicted)
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
650
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MITRKIWBJVJRAM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H14ClF3N4O2/c17-14-12(7-21-22-15(14)26)23-5-6-24(13(25)9-23)8-10-3-1-2-4-11(10)16(18,19)20/h1-4,7H,5-6,8-9H2,(H,22,26)
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| Chemical Name |
4-chloro-5-(3-oxo-4-(2-(trifluoromethyl)benzyl)piperazin-1-yl)pyridazin-3(2H)-one
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| Synonyms |
GFB-8438 GFB 8438 GFB8438
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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) |
DMSO : ~83.33 mg/mL (~215.46 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.38 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 20.8 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: ≥ 2.08 mg/mL (5.38 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 20.8 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: ≥ 2.08 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5856 mL | 12.9279 mL | 25.8558 mL | |
| 5 mM | 0.5171 mL | 2.5856 mL | 5.1712 mL | |
| 10 mM | 0.2586 mL | 1.2928 mL | 2.5856 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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