BAR-501
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MedKoo CAT#: 530595

CAS#: 1632118-69-4

Description: BAR-501 is a selective GPBAR1 agonist devoid of any FXR agonistic activity. BAR501 effectively reduced hepatic perfusion pressure and counteracted the vasoconstriction activity of norepinephrine. BAR501 rescues from endothelial dysfunction in rodent models of portal hypertension by exerting genomic and non-genomic effects on CSE, eNOS and ET-1 in liver sinusoidal cells.


Price and Availability

Size
Price

50mg
USD 450
500mg
USD 1950
5g
USD 7950
Size
Price

100mg
USD 650
1g
USD 3250
Size
Price

200mg
USD 1050
2g
USD 4650

BAR 501, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 530595
Name: BAR-501
CAS#: 1632118-69-4
Chemical Formula: C26H46O3
Exact Mass: 406.3447
Molecular Weight: 406.651
Elemental Analysis: C, 76.79; H, 11.40; O, 11.80


Synonym: BAR-501; BAR 501; BAR501.

IUPAC/Chemical Name: (3R,5S,6S,7S,8S,9S,10S,13R,14S,17R)-6-ethyl-17-((R)-5-hydroxypentan-2-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthrene-3,7-diol

InChi Key: DQBAHTQWQZRMFH-CRPAWOMZSA-N

InChi Code: InChI=1S/C26H46O3/c1-5-18-22-15-17(28)10-12-26(22,4)21-11-13-25(3)19(16(2)7-6-14-27)8-9-20(25)23(21)24(18)29/h16-24,27-29H,5-15H2,1-4H3/t16-,17-,18+,19-,20+,21+,22+,23+,24+,25-,26-/m1/s1

SMILES Code: C[C@H](CCCO)[C@H]1CC[C@@]2([H])[C@]3([H])[C@@H](O)[C@@H](CC)[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

GPBAR1 is a bile acids activated receptor expressed in entero-hepatic tissues. In the liver expression of GPBAR1 is restricted to sinusoidal and Kuppfer cells. In the systemic circulation vasodilation caused by GPBAR1 agonists is abrogated by inhibition of cystathione-γ-liase (CSE), an enzyme essential to the generation of hydrogen sulfide (H2S), a vasodilatory agent.


References

1: Renga B, Cipriani S, Carino A, Simonetti M, Zampella A, Fiorucci S. Reversal
of Endothelial Dysfunction by GPBAR1 Agonism in Portal Hypertension Involves a
AKT/FOXOA1 Dependent Regulation of H2S Generation and Endothelin-1. PLoS One.
2015 Nov 5;10(11):e0141082. doi: 10.1371/journal.pone.0141082. eCollection 2015.
PubMed PMID: 26539823; PubMed Central PMCID: PMC4634759.