Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.
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描述 | Rat CGRP-(8-37) TFA salt, a cholestanol-conjugated antagonist, accumulated in CLR(calcitonin receptor-like receptor)-containing endosomes and selectively inhibited CLR signaling in endosomes. CGRP8-37-cholestanol, but not unconjugated CGRP8-37, prevented sustained neuronal excitation. When injected intrathecally to mice, CGRP8-37-cholestanol inhibited nociceptive responses to intraplantar injection of capsaicin, formalin, or complete Freund's adjuvant more effectively than unconjugated CGRP8-37[3]. CGRP(8-37) is a truncated version of calcitonin gene-related peptide (CGRP) that binds to the CGRP receptor with similar affinity but does not activate the receptor and is a highly selective CGRP receptor antagonist. CGRP-(8-37) is effective in alleviating mechanical and thermal allodynia in a dose-dependent manner. The 50 nM dose is most efficacious for both forelimb and hindlimb responses. The period of efficacy is 10 min to onset for a duration of 20 min[4]. Intrathecal administration of 5 nmol or 10 nmol of CGRP-(8-37), but not 1 nmol, induces a significant increase in hindpaw withdrawal latency. Intrathecal administration of CGRP-(8-37) not only reverses the SP-induced decrease in latency to both withdrawal responses but also mediates a significant increase in response latency compared to basal levels[5]. |
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存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
0.31mL 0.06mL 0.03mL |
1.54mL 0.31mL 0.15mL |
3.08mL 0.62mL 0.31mL |
CAS号 | N/A |
分子式 | C140H225F3N42O43 |
分子量 | 3241.54 |
SMILES Code | O=C([C@H]([C@H](O)C)NC([C@@H](N)C(C)C)=O)N[C@@H](CC1=CNC=N1)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](C)C(NCC(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CO)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CO)C(NCC(NCC(N[C@@H](C(C)C)C(N[C@@H](C(C)C)C(N[C@@H](CCCCN)C(N[C@@H](CC(O)=O)C(N[C@@H](CC(N)=O)C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H](C(C)C)C(N3[C@@H](CCC3)C(N[C@](C(N[C@@H](CC(N)=O)C(N[C@@H](C(C)C)C(NCC(N[C@@H](CO)C(N[C@@H](CCC(O)=O)C(N[C@@H](C)C(N[C@H](C(N)=O)CC4=CC=CC=C4)=O)=O)=O)=O)=O)=O)=O)([C@H](O)C)[H])=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O |
MDL No. | N/A |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |