INT-777

CAS Number: 1199796-29-6


*

size

Price:            $0.00
Availability: In Stock
Cat No.: 1199796-29-6
Biological Description:
INT-777(S-EMCA) is a novel potent and selective TGR5 agonist with remarkable in vivo activity (EC50=0.82 uM).
IC50 value: 0.82 uM [1]
Target: TGR5 agonist
INT-777 shows a detergency power similar to CA (4), albeit with slightly lower water solubility. S-EMCA (8) is resistant to conjugation, with more than 90% of the compound being secreted into the bile in its unconjugated form after intravenous or intraduodenal infusion. S-EMCA is efficiently absorbed and undergoes enterohepatic cycling albeit with relatively little liver conjugation. S-EMCA (8) dramatically and dose-dependently induces the release of GLP-1 ex vivo. Along with these effects, we have recently demonstrated in a joint paper that the pharmacological targeting of TGR5 by S-EMCA (8) efficiently increases GLP-1 secretion in vivo.

Purity: >98%

Molecular formula: C27H46O5

Molecular Weight: 450.65

Storage Instructions: Two years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO

References: for more information, please visit http://www.ncbi.nlm.nih.gov