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INT-767 sodium, the sodium salt of INT767, is a novel and potent TGR5 (G-protein coupled)/Farnesoid X-activated receptor agonist with the potential to be used for the treatment of hepatic fibrosis. As a dual farnesoid X receptor/TGR5 agonist, it has EC50s of 30 and 630 nM, respectively.
| ln Vitro |
INT-767 is very stable to phase I and phase II enzymatic changes, does not inhibit cytochrome P450 enzymes, does not show cytotoxic effects in HepG2 cells, and does not block potassium channels associated to the human ether-a-go-go gene [2].
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| ln Vivo |
In db/m and db/db mice, INT-767 (10–20 mg/kg; i.p.; once daily for two weeks) lowers plasma total cholesterol and triglyceride levels [2].
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| Animal Protocol |
Animal/Disease Models: Male 8weeks old C57BKS/J db/db mice, control non-diabetic db/m mice [2]
Doses: 10, 20 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 2 weeks Experimental Results: Plasma total cholesterol and triglyceride levels were diminished. |
| References |
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| Additional Infomation |
See also: Int-767 (annotation moved to).
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| Molecular Formula |
C25H43NAO6S
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|---|---|
| Molecular Weight |
494.660098314285
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| Exact Mass |
494.267
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| CAS # |
1000403-03-1
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| Related CAS # |
1000403-03-1 (sodium);1000403-00-8 (free);
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| PubChem CID |
23712772
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
786
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| Defined Atom Stereocenter Count |
11
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| SMILES |
CC[C@@H]1[C@@H]2C[C@@H](CC[C@@]2([C@H]3CC[C@]4([C@H]([C@@H]3[C@@H]1O)CC[C@@H]4[C@H](C)CCOS(=O)(=O)[O-])C)C)O.[Na+]
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| InChi Key |
TXIWHUPIUUZFFK-PMWRKVJASA-M
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| InChi Code |
InChI=1S/C25H44O6S.Na/c1-5-17-21-14-16(26)8-11-25(21,4)20-9-12-24(3)18(6-7-19(24)22(20)23(17)27)15(2)10-13-31-32(28,29)30;/h15-23,26-27H,5-14H2,1-4H3,(H,28,29,30);/q;+1/p-1/t15-,16-,17-,18-,19+,20+,21+,22+,23-,24-,25-;/m1./s1
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| Chemical Name |
sodium;[(3R)-3-[(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]butyl] sulfate
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| Synonyms |
INT 767 INT767INT-767 INT-767 Free
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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 (~202.16 mM)
H2O : ~100 mg/mL (~202.16 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.05 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 (5.05 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 (5.05 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 (101.08 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 | 2.0216 mL | 10.1080 mL | 20.2159 mL | |
| 5 mM | 0.4043 mL | 2.0216 mL | 4.0432 mL | |
| 10 mM | 0.2022 mL | 1.0108 mL | 2.0216 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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