| 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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| 250mg |
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| 500mg |
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Purity: ≥98%
CFTRinh-172 (also known as CFTR Inhibitor172; CFTR-Inh 172; CFTR inhibitor 172) is a potent, voltage-independent, and selective inhibitor of CFTR (Cystic fibrosis transmembrane conductance regulator) with potential anti-fibrotic and anti-diarrhea effects. It inhibits CFTR with a Ki of 300 nM, and exhibits little/no effects on MDR1, ATP-sensitive K+ channels, or other transporters. CFTRinh-172 could reversibly inhibit CFTR short-circuit current in less than 2 minutes in a voltage-independent manner.
| ln Vitro |
Inhibition by CFTR(inh)-172 is complete in around 10 minutes (t1/2=4 min) and is reversed after roughly 5 minutes at t1/2. CFTRinh-172 suppresses FRT after 24 hours at doses up to 100 μM[1] Cells are non-toxic. CFTR(inh)-172 does not modify the CFTR unitary conductance (8 pS) but reduces the open probability by >90% at Ki=0.6 μM. This effect is due to increasing the average channel off time without changing the average channel on time. The Ki value of wild-type, G551D, and G1349D CFTR for blocking Cl- current is approximately 0.5 μM; however, for vF508 CFTR, the Ki is drastically lowered to 0.2 μM [2].
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| ln Vivo |
In mice, cholera toxin-induced small intestinal fluid secretion was reduced by almost 90% after a single intraperitoneal injection of CFTR(inh)-172 (250 μg/kg) within 6 hours. In mouse models, CFTR(inh)-172 is not harmful at high concentrations. While inactive CFTRinh-172 analogues do not suppress fluid secretion, CFTRinh-172 dramatically decreases fluid secretion into the saline control circuit [1].
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| Animal Protocol |
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| References |
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| Additional Infomation |
See also: CFTRinh-172 (annotation moved to).
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| Molecular Formula |
C18H10F3NO3S2
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| Molecular Weight |
409.4
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| Exact Mass |
409.005
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| CAS # |
307510-92-5
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| Related CAS # |
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| PubChem CID |
1554208
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
555.7±60.0 °C at 760 mmHg
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| Flash Point |
289.9±32.9 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.698
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| LogP |
4.51
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
657
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC(=C1)N2C(=O)/C(=C/C3=CC=C(C=C3)C(=O)O)/SC2=S)C(F)(F)F
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| InChi Key |
JIMHYXZZCWVCMI-ZSOIEALJSA-N
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| InChi Code |
InChI=1S/C18H10F3NO3S2/c19-18(20,21)12-2-1-3-13(9-12)22-15(23)14(27-17(22)26)8-10-4-6-11(7-5-10)16(24)25/h1-9H,(H,24,25)/b14-8-
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| Chemical Name |
4-{[(5Z)-4-Oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]methyl}benzoic acid
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.11 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (6.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4426 mL | 12.2130 mL | 24.4260 mL | |
| 5 mM | 0.4885 mL | 2.4426 mL | 4.8852 mL | |
| 10 mM | 0.2443 mL | 1.2213 mL | 2.4426 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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