GFB-8438
Based on 1 Customer Validation
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 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.
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- Purity: 99.74%
- CAS No.: 2304549-73-1
- 화학식: C16H14ClF3N4O2
- 분자량:386.76
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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hTRPC5 0.18 μM (IC50) |
hTRPC4 0.29 μM (IC50) |
rTRPC5 0.18 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>30 μM
Compound: GFB-8438
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Inhibition of human Nav1.5 stably expressed in CHO cells measured at holding potential of -80 mV by manual patch clamp assay
Inhibition of human Nav1.5 stably expressed in CHO cells measured at holding potential of -80 mV by manual patch clamp assay
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[PMID: 31749913] |
| HEK293 | IC50 |
>30 μM
Compound: GFB-8438
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Inhibition of OAG-activated human TRPC6 channel expressed in HEK293 cells by Q-patch clamp assay
Inhibition of OAG-activated human TRPC6 channel expressed in HEK293 cells by Q-patch clamp assay
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[PMID: 31749913] |
| HEK293 | IC50 |
0.18 μM
Compound: GFB-8438
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Inhibition of rosiglitazone-activated human TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay
Inhibition of rosiglitazone-activated human TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay
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[PMID: 31749913] |
| HEK293 | IC50 |
0.18 μM
Compound: GFB-8438
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Inhibition of rosiglitazone-activated rat TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay
Inhibition of rosiglitazone-activated rat TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay
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[PMID: 31749913] |
| HEK293 | IC50 |
0.28 μM
Compound: GFB-8438
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Inhibition of human TRPC5 channel expressed in HEK293 cells assessed as decrease in current amplitude treated for 3 mins measured between +80 mV and -80 mV by manual patch clamp assay
Inhibition of human TRPC5 channel expressed in HEK293 cells assessed as decrease in current amplitude treated for 3 mins measured between +80 mV and -80 mV by manual patch clamp assay
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[PMID: 31749913] |
| HEK293 | IC50 |
0.29 μM
Compound: GFB-8438
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Inhibition of Englerin-activated human TRPC4 channel expressed in HEK293 cells by Q-patch clamp assay
Inhibition of Englerin-activated human TRPC4 channel expressed in HEK293 cells by Q-patch clamp assay
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[PMID: 31749913] |
| HEK293 | IC50 |
8.7 μM
Compound: GFB-8438
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Inhibition of human ERG stably expressed in HEK293 cells measured at holding potential of -90 mV by manual patch clamp assay
Inhibition of human ERG stably expressed in HEK293 cells measured at holding potential of -90 mV by manual patch clamp assay
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[PMID: 31749913] |
Pretreatment of mouse podocyte with GFB-8438 (1 μM for 30 min), followed by incubation with protamine sulfate, effectively blocked synaptopodin loss and cytoskeletal remodeling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GFB-8438 (1 mg/kg; i.v.) treatment shows the?Cl,?VSS,?and ?t1/2?were?31?mL/min/kg,?1.17?L/kg,?and?0.5 hours, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley rats (DOCA-salt rat model of FSGS)[1]
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Dosage:30 mg/kg
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Administration:s.c.; daily for 3 weeks
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Result:Significant reduction in urine protein concentrations.
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Animal Model:6-8 weeks old male SD rats[1]
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Dosage:1 mg/kg
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Administration:i.v. (Pharmacokinetic Analysis)
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Result:The Cl, Vss, and t1/2 were 31 mL/min/kg, 1.17 L/kg, and 0.5 hours, respectively.
Chemical Information
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CAS No. 2304549-73-1
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Appearance Solid
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분자량 386.76
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화학식 C16H14ClF3N4O2
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Color Off-white to light yellow
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SMILES
O=C1CN(C2=C(Cl)C(NN=C2)=O)CCN1CC3=CC=CC=C3C(F)(F)F
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 83.33 mg/mL (215.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5856 mL | 12.9279 mL | 25.8558 mL | 64.6396 mL |
| 5 mM | 0.5171 mL | 2.5856 mL | 5.1712 mL | 12.9279 mL | |
| 10 mM | 0.2586 mL | 1.2928 mL | 2.5856 mL | 6.4640 mL | |
| 15 mM | 0.1724 mL | 0.8619 mL | 1.7237 mL | 4.3093 mL | |
| 20 mM | 0.1293 mL | 0.6464 mL | 1.2928 mL | 3.2320 mL | |
| 25 mM | 0.1034 mL | 0.5171 mL | 1.0342 mL | 2.5856 mL | |
| 30 mM | 0.0862 mL | 0.4309 mL | 0.8619 mL | 2.1547 mL | |
| 40 mM | 0.0646 mL | 0.3232 mL | 0.6464 mL | 1.6160 mL | |
| 50 mM | 0.0517 mL | 0.2586 mL | 0.5171 mL | 1.2928 mL | |
| 60 mM | 0.0431 mL | 0.2155 mL | 0.4309 mL | 1.0773 mL | |
| 80 mM | 0.0323 mL | 0.1616 mL | 0.3232 mL | 0.8080 mL | |
| 100 mM | 0.0259 mL | 0.1293 mL | 0.2586 mL | 0.6464 mL |
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