INT-777 free base · Synonyms: S-EMCA
INT-777 is a potent TGR5 agonist.
For research use only. Not for human or veterinary use.
INT-777 structure
CAS No.: 1199796-29-6
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 25 mg | USD 395.00 | BP-01849-25mg | In stock | Get quote |
| 50 mg | USD 550.00 | BP-01849-50mg | In stock | Get quote |
| 100 mg | USD 795.00 | BP-01849-100mg | In stock | Get quote |
| 250 mg | USD 1,380.00 | BP-01849-250mg | In stock | Get quote |
| 500 mg | USD 2,120.00 | BP-01849-500mg | In stock | Get quote |
| 1 g | USD 3,280.00 | BP-01849-1g | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM.
Biological activity
In Vitro INT-777 is a novel potent and selective TGR5 agonist with remarkable in vivo activity[1]. INT-777 (3 μM) increases ATP production in the human enteroendocrine cell line NCI-H716 in a cAMP-dependent manner. INT-777 (10 μM) lowers Isc and increases TEER when added on the serosal side of seromuscular stripped distal colon segments. INT-777 effect on basal secretion is reduced in neuron-free and TTX-treated mucosal-submucosal preparations. In Vivo INT-777 (1 μM/min/kg, p.o.) has a potent choleretic effect, prevents carboxyl CoA activation and subsequent conjugation, thereby favoring its chole-hepatic shunt pathway with a ductular absorption and a potent choleretic effect in HF-fed TGR5-Tg male mice. INT-777 (30 mg/kg/day, p.o.) increases energy expenditure and reduces hepatic steatosis and obesity upon high-fat feeding in TGR5-Tg mice.
Identifiers
- SMILES
-
O[C@@H]1CC[C@@]2(C)[C@@]([C@@H](CC)[C@@H](O)[C@]3([H])[C@]2([H])C[C@H](O)[C@@]4(C)[C@@]3([H])CC[C@@H]4[C@H](C)C[C@H](C)C(O)=O)([H])C1 - InChIKey
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NPBCMXATLRCCLF-IRRLEISYSA-N
Specifications
- MW (average)
- 450.6511
- Formula
- C27H46O5
- CAS No.
- 1199796-29-6
- Physical state
- Solid
- Color
- white to yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month
Solubility
Soluble in DMSO : 100 mg/mL Ethanol : ≥ 50 mg/mL