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BIM 23042

Catalog No.GC17080

Antagonist of neuromedin B receptor,selective

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BIM 23042 Chemical Structure

Cas No.: 111857-96-6

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1mg
$195.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Ki: 49 ±14 nM for neuromedin B-induced endpoint in huNMBR cells

Neuromedin B, a mammalian peptide of the bombesinlike peptide family sharing amino acid homology with its amphibian counterpart ranatensin, elicits a diverse array of biological responses in central and peripheral tissues. BIM 23042 [D-Nal-Cys-Tyr- D-Trp-Lys-Val-Cys-Nal-NH2] is a selective neuromedin B antagonist.

In vitro: BIM 23042 has a l00-fold greater affinity for BB1 receptors than BB2 receptors. The submaximal mobilisation observed with neuromedin B (1 nM) was abolished by BIM 23042 but restored with a subsequently higher concentration of neuromedin B (1 μM). BIM 23042 competitively inhibited neuromedin B-induced endpoint in huNMBR cells with a Ki of 49 ±14 nM [1].

In vivo: In cat upper GI tract, SSocta, at concentrations of 10 mM, did not influence the smooth muscle tone but shifted NMB concentration response to the right yielding (Ki=1.7±0.8 mM). Ssocta inhibited both NMB- and GRP-induced contractions on the esophagus. the NMB-receptor antagonist SSocta had no effect on circular fundic muscle indicating the absence of this receptor subtype on fundus. [2].

Clinical trial: Up to now, BIM 23042 is still in the preclinical development stage.

References:
[1] Ryan RR, Taylor JE, Daniel JL, Cowan A.  Pharmacological profiles of two bombesin analogues in cells transfected with human neuromedin B receptors. Eur J Pharmacol. 1996 Jun 13;306(1-3):307-14.
[2] Milusheva EA, Kortezova NI, Mizhorkova ZN, Papasova M, Coy DH, Bálint A, Vizi ES, Varga G.  Role of different bombesin receptor subtypes mediating contractile activity in cat upper gastrointestinal tract. Peptides. 1998;19(3):549-56.

Chemical Properties

Cas No. 111857-96-6 SDF
Canonical SMILES CC([C@@](/N=C(O)/[C@](/N=C(O)/[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@@](N)([H])C1=CC2=CC=CC=C2C=C1)([H])CS)([H])CC3=CC=C(O)C=C3)([H])CC4=CNC5=CC=CC=C45)([H])CCCCN)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CC6=CC7=CC=CC=C7C=C6)([H])CS)C
Formula C62H73N11O9S2 M.Wt 1180.44
Solubility Soluble to 1 mg/ml in 0.1% acetic acid Storage Desiccate at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 0.8471 mL 4.2357 mL 8.4714 mL
5 mM 0.1694 mL 0.8471 mL 1.6943 mL
10 mM 0.0847 mL 0.4236 mL 0.8471 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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