BIBS 39 - 10mM in DMSO , CAS No.133085-33-3

CAS: 133085-33-3 Cat. No.: B656069 Summenformel: C₃₂H₃₆N₄O₃ Molekulargewicht: 524.65 PubChem CID: 131590

QUALITÄT & REINHEIT 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.Target: Angiotensin Receptor in vitro: BIBS 39 displaces [125I] AII from its specific binding sites with a Ki value of 29 ± 7 nM for the AII subtype 1 (AT1) receptor and a Ki value of 480 ± 110 nM for the AII subtype 2 (AT2) receptor. BIBS 222 shows a Ki value of 20 ± 7 nM for the AT1 subtype and a Ki value of 730 ± 170 nM for the AT2 subtype. BIBS 39 is 17 times more selective for the AT1 subtype and BIBS 222 37 times. BIBS 39 shifts the AII concentration-contractile response curves in isolated rabbit aorta to the right in a parallel fashion.in vivo: In pithed rats, BIBS 39 dependently shifts the dose-response curve of AII to the right without affecting the maximal response. BIBS 222 also causes parallel shifts to the right but a significant reduction of the maximal responses was observed at 3 and 10 mg/kg i.v. These results show that the benzimidazole derivatives BIBS 39 is a potent and selective AII receptor antagonists. Substitution with a benzimidazole moiety results into a considerable loss of selectivity for the AT1 receptor subtype compared with an imidazole moiety as, for instance, in DuP 753.BIBS 39 is a new nonpeptide angiotensin receptor blockers that has affinity for both AT1- and AT2-receptors, is also a potent antagonist of the cardiovascular effects of AII in pithed rabbits.

Spezifikationen

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.\nTarget: Angiotensin Receptor in vitro: BIBS 39 displaces [125I] AII from its specific binding sites with a Ki value of 29 ± 7 nM for the AII subtype 1 (AT1) receptor and a Ki value of

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Namen und Kennungen

Isomere SMILES

CCCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2)NC(=O)NC5CCCCC5

Alternative CAS-Nummer

133085-33-3

PubChem CID

131590

MeSH-Eintrag

4'-((2-n-butyl-6-cyclohexylaminocarbonylaminobenzimidazole-1-yl)methyl)biphenyl-2-carboxylic acid;BIBS 39;BIBS-39

Molekulargewicht

524.65

Zugehörige Ziele (menschlich)

AGTR1 Tclin Type-1 angiotensin II receptor (1 Activities)

Discover Target: AGTR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)