b1 receptor

ELN-441958 is a potent, neutral antagonist of the B1 receptor, inhibiting the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with a Ki of 0.26 nM. ELN-441958 (ELN 441958) is highly selective for B1 over B2 receptors.

SSR240612 is a potent, orally active, specific non-peptide bradykinin B1 receptor antagonist (Kis = 0.48-0.73 nM for B1 receptors and 358-481 nM for B2 receptors, respectively).

[Des-Arg9]-Bradykinin ([Des-Arg9]-Bradykinin(2TFA))(2TFA) is an agonist of Bradykinin (B1) receptor.

Bradykinin B1 Receptor Antagonist 1 (compound 6B) is a potent bradykinin B1 antagonist that can cross the blood-brain barrier. It holds potential for pain research.

MK-0686 is an orally available bradykinin B1 receptor antagonist with potential anti-inflammatory activity.

Safotibant (LF-22-0542) is a bradykinin B1 receptor antagonist with anti-inflammatory and analgesic activity for the topical treatment of diabetic macular edema.

Lys-[Des-Arg9]Bradykinin acetate is an endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]-Bradykinin.

PU02 (6-[(1-Naphthalenylmethyl)thio]-9H-purine) is a potent and selective antagonist of 5-HT3 receptor.

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate is a potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

EG00229 is a neuropilin 1 (NRP1) receptor antagonist that selectively inhibits the binding of VEGF-A to the NRP1 b1 domain with an IC50 value of 3 μM. It does not affect the binding of VEGF-A to other receptors, such as VEGFR-1 and VEGFR-2.

BLT-1 is a scavenger receptor BI (SR-BI)inhibitor.

FR167344 free base is an orally active, nonpeptide antagonist of the bradykinin receptor B2, exhibiting high-affinity binding (IC50: 65 nM) and showing no binding affinity for the B1 receptor.

ITX5061 is a type II inhibitor of p38 MAPK and an antagonist of scavenger receptor B1 (SRB1), used for studying hepatitis C virus infection.

BI-113823 is an orally active and selective bradykinin B1 receptor antagonist. It alleviates mechanical hyperalgesia induced by complete Freund's adjuvant in rats. BI-113823 is applicable for research on chronic inflammatory pain.

[Des-Arg10]-HOE I40 TFA is a potent antagonist of the bradykinin B1 receptor.

ERα degrader7 (Compound B1) is a potent ERα degrader, exhibiting an IC50 of 14.6 nM and a DC50 of 9.7 nM. This compound demonstrates excellent antitumor activity, indicating its potential as a selective estrogen receptor degrader (SERD) for breast cancer research.

NVP-SAA164 is a nonpeptide bradykinin B1 receptor antagonist agent.

Ex26 (S1P1-IN-Ex26) is a selective and potent sphingosine 1-phosphate receptor 1 (S1P1) antagonist that disrupts SR-B1-S1PR1 interactions and inhibits S1P-S1PR1 signaling. Ex26 is used in experimental autoimmune encephalomyelitis, atherosclerosis, and gastric cancer.

Napyradiomycin A1is a fungal metabolite originally isolated fromC. rubraand has diverse biological activities.1,2It is active againstS. aureus,M. luteus,B. anthracis,C. bovis, andM. smegmatis(MICs = 1.56-12.5 μg/ml).1Napyradiomycin A1is an estrogen receptor antagonist (IC50= 4.2 μM in rat uterine homogenates).2It also inhibits mitochondrial NADH:ubiquinone oxidoreductase (complex I) and succinate:ubiquinone oxidoreductase (complex II) activities in bovine heart homogenates (IC50s = 20 and 9.7 μM, respectively).3 1.Shiomi, K., Iinuma, H., Hamada, M., et al.Novel antibiotics napyradiomycins. Production, isolation, physico-chemical properties and biological activityJ. Antibiot. (Tokyo)39(4)487-493(1986) 2.Hori, Y., Abe, Y., Shigematsu, N., et al.Napyradiomycins A and B1: Non-steroidal estrogen-receptor antagonists produced by a StreptomycesJ. Antibiot. (Tokyo)46(12)1890-1893(1993) 3.Yamamoto, K., Tashiro, E., Motohashi, K., et al.Napyradiomycin A1, an inhibitor of mitochondrial complexes I and IIJ. Antibiot. (Tokyo)65(4)211-214(2012)

Lys-[Des-Arg9]Bradykinin TFA is a naturally occurring kinin that serves as a potent and highly selective agonist for the bradykinin B1 receptor, demonstrating binding affinities (K i values) of 0.12 nM, 1.7 nM, and 0.23 nM for the human, mouse, and rabbit B1 receptors, respectively. This compound exhibits low inhibitory activity on B2 receptors [1] [2].

B 9430 is a potent bradykinin B1/B2 receptor antagonist [1].

Laminin (925-933) (TFA) is a peptide corresponding to the 925-933 sequence of the Laminin B1 chain, known to bind the laminin receptor [1].

Lys-(Des-Arg9,Leu8)-Bradykinin is a selective antagonist of the bradykinin B1 receptor [1].

[Des-Arg10]-HOE 140 is a bioactive peptide that functions as a potent B1 bradykinin receptor antagonist.