H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2
H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2 Basic information
- Product Name:
- H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2
- Synonyms:
-
- 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
- (D-2-Nal5,Cys6
- BIM-23042, DC-13-217
- BIM 23042
- 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
- (D-2-NAL5,CYS6·11,TYR7,D-TRP8,VAL10,2-NAL12)-SOMATOSTATIN
- (D-2-Nal?,Cys?·??,Tyr?,D-Trp?,Val??,2-Nal??)-Somatostatin-14 (5-12) amide trifluoroacetate salt
- CAS:
- 111857-96-6
- MF:
- C63H73N11O9S2
- MW:
- 1192.45
- Mol File:
- 111857-96-6.mol
H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2 Chemical Properties
- 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)
H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2 Usage And Synthesis
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. |
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.
H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2Supplier
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H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2(111857-96-6)Related Product Information
- H-D-2-NAL-CYS-TYR-D-TRP-LYS-VAL-CYS-2-NAL-NH2
- 1-NAPHTHALEN-2-YL-ETHYLAMINE
- 3-(NAPHTHALEN-2-YL)PROPAN-1-AMINE
- 2-NAPHTHALEN-2-YL-ETHYLAMINE
- (S)-(-)-1-(2-Naphthyl)ethylamine
- SOMATOSTATIN-28 (1-14)
- (D-PHE5,CYS6,11,N-ME-D-TRP8)-SOMATOSTATIN-14 (5-12) AMIDE
- SOMATOSTATIN 28, CYCLIC
- CYCLO(7-AMINOHEPTANOYL-PHE-D-TRP-LYS-THR[BZL])
- H-PHE-TRP-LYS-THR-PHE-THR-SER-CYS-OH