| Identification | Back Directory | [Name]
H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2 | [CAS]
111857-96-6 | [Synonyms]
BIM 23042
(D-2-Nal5,Cys6
BIM-23042, DC-13-217
H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2
(D-2-NAL5,CYS6'11,TYR7,D-TRP8,VAL10,2-NAL12)-SOMATOSTATIN-14 (5-12) AMIDE
L-Alaninamide, 3-(2-naphthalenyl)-D-alanyl-L-cysteinyl-L-tyrosyl-D-tryptophyl-L-lysyl-L-valyl-L-cysteinyl-3-(2-naphthalenyl)-, cyclic (2→7)-disulfide | [Molecular Formula]
C63H73N11O9S2 | [MDL Number]
MFCD00237258 | [MOL File]
111857-96-6.mol | [Molecular Weight]
1192.45 |
| Chemical Properties | Back Directory | [Boiling point ]
1554.2±65.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
-15°C
| [solubility ]
Soluble to 1 mg/ml in 0.1% acetic acid | [form ]
solid | [pka]
9.90±0.15(Predicted) | [color ]
White | [Sequence]
{DNal}-Cys-Tyr-{DTrp}-Lys-Val-Cys-{Nal}-NH2 (Disulfide bridge:Cys2-Cys7) |
| Hazard Information | Back Directory | [Uses]
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin?B?(HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca2+ release[1][2][3]. | [Biological Activity]
ki: 49 ±14 nm for neuromedin b-induced endpoint in hunmbr cellsneuromedin 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]
BIM 23042 (10 μg; IV; a single bolus) attenuates neurogenic swelling and thermal and mechanical sensitization[2].
| Animal Model: | Mice were 25-30 g male C57BL/6[2] | | Dosage: | 10 μg | | Administration: | IV; a single bolus | | Result: | Attenuated neurogenic swelling and thermal and mechanical sensitization. |
| [storage]
Desiccate at -20°C | [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. |
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