Erenumab  (Synonyms: AMG-334)

Erenumab (AMG-334) is a fully human monoclonal antibody. Erenumab inhibits the calcitonin gene-related peptide (CGRP) receptor. Erenumab prevents the increase in dermal blood flow in cynomolgus monkeys. Erenumab can be used in the research of episodic migraine^[1][2][3].

Human IgG2 lambda

Human IgG2 lambda, Isotype Control

Human

CALCRL/CGRPR

Erenumab (1-100 nM) competitively inhibits the vasodilatory effect induced by aCGRP, with a pA₂ of 9.00 in cerebral arteries and an apparent pK_B of 7.50 in meningeal arteries, indicating that it is more potent in cerebral arteries^[2].
Erenumab (0.5 pM-10 μM, 3 h) competes with [¹²⁵I]-CGRP for binding to human CGRP receptors, with a K_i value of 0.02 nM. In cell-based functional assays (human CGRP receptors), AMG 334 fully inhibits CGRP-stimulated cyclic adenosine monophosphate (cAMP) production, with an IC₅₀ of 2.3 nM^[3].
Erenumab (0.5 pM-10 μM, 3 h) exhibits antagonistic potency at cynomolgus monkey CGRP receptors, with an IC₅₀ of 5.7 nM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Erenumab (0.1-30 mg/kg, i.v., single dose) dose-dependently inhibits capsaicin-induced increases in dermal blood flow in cynomolgus monkeys^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

10203  [NCBI]

Q16602

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

145.5 kDa

1582205-90-0

Liquid

Colorless to light yellow

[Erenumab]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  Human IgG2 lambda

• [1]. Shi L, et al. Pharmacologic Characterization of AMG 334, a Potent and Selective Human Monoclonal Antibody against the Calcitonin Gene-Related Peptide Receptor. J Pharmacol Exp Ther. 2016 Jan;356(1):223-31.  [Content Brief]

  [2]. Reuter U, et al. Erenumab versus topiramate for the prevention of migraine - a randomised, double-blind, active-controlled phase 4 trial. Cephalalgia. 2022;42(2):108-118.  [Content Brief]

  [3]. Ohlsson L, et al. Erenumab (AMG 334), a monoclonal antagonist antibody against the canonical CGRP receptor, does not impair vasodilatory or contractile responses to other vasoactive agents in human isolated cranial arteries. Cephalalgia. 2019;39(14):1745-1752.  [Content Brief]