Home > Products > Screening Compounds P17080 > alpha-CGRP (human)

alpha-CGRP (human)

Catalog Number: EVT-242155

CAS Number: 90954-53-3

Molecular Formula: C163H267N51O49S2

Molecular Weight: 3791.3 g/mol

The product is for non-human research only. Not for therapeutic or veterinary use.

Inquire Now

Product Introduction

Description

Alpha-Calcitonin Gene-Related Peptide (alpha-CGRP) is a neuropeptide with a wide range of physiological effects. It is a member of the calcitonin family of peptides and is involved in various processes such as vasodilation, nociception, and modulation of immune responses. The peptide is widely distributed throughout the central and peripheral nervous systems and has been implicated in the regulation of vascular tone and as a mediator in inflammatory and pain pathways8.

Mechanism of Action

Alpha-CGRP exerts its effects primarily through the activation of the CGRP1 receptor subtype. This receptor is coupled to the adenylate cyclase enzyme, leading to an increase in intracellular cyclic AMP (cAMP) upon activation. The rise in cAMP levels ultimately results in a cascade of intracellular events that modulate cellular functions. For instance, in the context of vasodilation, alpha-CGRP induces relaxation of vascular smooth muscle cells, leading to an increase in blood flow2 3. Additionally, alpha-CGRP has been shown to have a role in the auditory system, where it affects the activity of cochlear sensory neurons, suggesting a postsynaptic effect on cochlear neurons via its release from lateral olivocochlear terminals1.

Applications in Various Fields

Auditory System

Alpha-CGRP has been implicated in the modulation of sound-evoked activity in the cochlear nerve. Studies using alphaCGRP-null mice have shown that while cochlear threshold sensitivity and resistance to acoustic injury remain normal, there is a significant abnormality in the growth of cochlear neural responses with increasing stimulus level. This suggests a selective effect on cochlear neurons, providing evidence for the functional role of the lateral olivocochlear system in the auditory periphery1.

Vascular System

In the vascular system, alpha-CGRP is a potent vasodilator, particularly in human mesenteric vasculature. It has been found to be more potent than sodium nitroprusside in evoking dose-dependent falls in perfusion pressure. This indicates that alpha-CGRP may preferentially act on arterioles rather than large arteries and could have therapeutic potential in conditions involving vascular constriction2. Additionally, alpha-CGRP has been shown to counteract vasoconstriction in human subarachnoid hemorrhage, suggesting its utility in managing cerebrovascular tone post-hemorrhage5.

Cardiovascular System

In cardiovascular research, alpha-CGRP has been demonstrated to have vasodilatory effects in the coronary vasculature, with species-specific variations in its effects on heart rate. For example, in the rat heart, alpha-CGRP elicited increases in heart rate, whereas it did not alter heart rate in the rabbit heart6.

Antagonism and Therapeutic Potential

The development of CGRP antagonists, such as human alpha-CGRP-(8-37), has provided tools for understanding the physiological roles of alpha-CGRP and for potential therapeutic applications. These antagonists have been shown to inhibit the vasodilator effects of alpha-CGRP, suggesting their potential use in conditions where modulation of CGRP's effects is desired3 7 8. The binding profile of these antagonists has been studied in various tissues, providing insights into the distribution and characteristics of CGRP receptors9.

Properties

CAS Number

90954-53-3

Product Name

alpha-CGRP (human)

IUPAC Name

(3S)-4-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-[[(2R)-2-[[(2S)-2-aminopropanoyl]amino]-3-sulfanylpropanoyl]amino]-4-oxobutanoic acid

Molecular Formula

C163H267N51O49S2

Molecular Weight

3791.3 g/mol

InChI

InChI=1S/C163H269N51O49S2/c1-73(2)52-97(186-116(226)65-179-131(233)82(18)183-139(241)98(53-74(3)4)193-137(239)94(44-35-49-176-162(171)172)188-142(244)101(57-91-62-175-72-182-91)199-159(261)128(88(24)221)213-156(258)123(79(13)14)207-151(253)110(71-265)204-160(262)126(86(22)219)210-133(235)84(20)185-157(259)125(85(21)218)211-147(249)105(61-119(229)230)198-150(252)109(70-264)203-130(232)81(17)166)140(242)194-99(54-75(5)6)141(243)202-108(69-217)149(251)190-95(45-36-50-177-163(173)174)138(240)201-106(67-215)134(236)180-63-115(225)178-64-118(228)205-121(77(9)10)155(257)208-122(78(11)12)154(256)191-93(43-32-34-48-165)136(238)196-102(58-112(167)222)144(246)197-103(59-113(168)223)143(245)195-100(56-90-40-29-26-30-41-90)145(247)209-124(80(15)16)161(263)214-51-37-46-111(214)152(254)212-127(87(23)220)158(260)200-104(60-114(169)224)146(248)206-120(76(7)8)153(255)181-66-117(227)187-107(68-216)148(250)189-92(42-31-33-47-164)135(237)184-83(19)132(234)192-96(129(170)231)55-89-38-27-25-28-39-89/h25-30,38-41,62,72-88,92-111,120-128,215-221,264-265H,31-37,42-61,63-71,164-166H2,1-24H3,(H2,167,222)(H2,168,223)(H2,169,224)(H2,170,231)(H,175,182)(H,178,225)(H,179,233)(H,180,236)(H,181,255)(H,183,241)(H,184,237)(H,185,259)(H,186,226)(H,187,227)(H,188,244)(H,189,250)(H,190,251)(H,191,256)(H,192,234)(H,193,239)(H,194,242)(H,195,245)(H,196,238)(H,197,246)(H,198,252)(H,199,261)(H,200,260)(H,201,240)(H,202,243)(H,203,232)(H,204,262)(H,205,228)(H,206,248)(H,207,253)(H,208,257)(H,209,247)(H,210,235)(H,211,249)(H,212,254)(H,213,258)(H,229,230)(H4,171,172,176)(H4,173,174,177)/t81-,82-,83-,84-,85+,86+,87+,88+,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,120-,121-,122-,123-,124-,125-,126-,127-,128-/m0/s1

InChI Key

DNKYDHSONDSTNJ-XJVRLEFXSA-N

SMILES

CC(C)CC(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCNC(=N)N)C(=O)NC(CO)C(=O)NCC(=O)NCC(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NC(CC(=O)N)C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)C)C(=O)N2CCCC2C(=O)NC(C(C)O)C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NCC(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C)C(=O)NC(CC3=CC=CC=C3)C(=O)N)NC(=O)CNC(=O)C(C)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC4=CN=CN4)NC(=O)C(C(C)O)NC(=O)C(C(C)C)NC(=O)C(CS)NC(=O)C(C(C)O)NC(=O)C(C)NC(=O)C(C(C)O)NC(=O)C(CC(=O)O)NC(=O)C(CS)NC(=O)C(C)N

Canonical SMILES

Isomeric SMILES

C[C@H]([C@@H](C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C(C)C)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC(=O)CNC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC4=CN=CN4)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CS)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)N)O

Product FAQ

Q1: How Can I Obtain a Quote for a Product I'm Interested In?

To receive a quotation, send us an inquiry about the desired product.
The quote will cover pack size options, pricing, and availability details.
If applicable, estimated lead times for custom synthesis or sourcing will be provided.
Quotations are valid for 30 days, unless specified otherwise.

Q2: What Are the Payment Terms for Ordering Products?

New customers generally require full prepayment.
NET 30 payment terms can be arranged for customers with established credit.
Contact our customer service to set up a credit account for NET 30 terms.
We accept purchase orders (POs) from universities, research institutions, and government agencies.

Q3: Which Payment Methods Are Accepted?

Preferred methods include bank transfers (ACH/wire) and credit cards.
Request a proforma invoice for bank transfer details.
For credit card payments, ask sales representatives for a secure payment link.
Checks aren't accepted as prepayment, but they can be used for post-payment on NET 30 orders.

Q4: How Do I Place and Confirm an Order?

Orders are confirmed upon receiving official order requests.
Provide full prepayment or submit purchase orders for credit account customers.
Send purchase orders to sales@EVITACHEM.com.
A confirmation email with estimated shipping date follows processing.

Q5: What's the Shipping and Delivery Process Like?

Our standard shipping partner is FedEx (Standard Overnight, 2Day, FedEx International Priority), unless otherwise agreed.
You can use your FedEx account; specify this on the purchase order or inform customer service.
Customers are responsible for customs duties and taxes on international shipments.

Q6: How Can I Get Assistance During the Ordering Process?

Reach out to our customer service representatives at sales@EVITACHEM.com.
For ongoing order updates or questions, continue using the same email.
Remember, we're here to help! Feel free to contact us for any queries or further assistance.

Quick Inquiry

Note: Kindly utilize formal channels such as professional, corporate, academic emails, etc., for inquiries. The use of personal email for inquiries is not advised.