AC 187 TFA is a potent and orally bioactive amylin receptor antagonist (inhibitor) with IC50 of 0.48 nM and a Ki of 0.275 nM. AC 187 TFA is more selective for amylin receptors than calcitonin and CGRP receptors. AC 187 TFA is neuro-protection.

Physicochemical Properties

Molecular Formula	C129H206F3N37O42
Molecular Weight	3004.27
Related CAS #	AC 187;151804-77-2
Appearance	White to off-white solid powder
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	IC50: 0.48 nM (amylin receptor)
ln Vitro	Amyloidβ protein (Aβ)-induced neurotoxicity is inhibited by AC 187. The neuronal survival of cultures treated with AC 187 prior to exposure to Aβ is markedly enhanced[1]. Aβ-induced apoptotic cell death is mediated by initiator and effector caspases, both of which are attenuated by AC187[1].
ln Vivo	In hyperinsulinemic clamps in Sprague-Dawley (HSD) rats, AC 187 (30 mg/mL) raises glucagon levels, speeds up gastric emptying of liquids, and causes an inflated post-challenge glycemia[2].
References	[1]. Antagonist of the amylin receptor blocks beta-amyloid toxicity in rat cholinergic basal forebrain neurons. J Neurosci. 2004 Jun 16;24(24):5579-84. [2]. Role of endogenous amylin in glucagon secretion and gastric emptying in rats demonstrated with the selective antagonist, AC187. Regul Pept. 2006 Dec 10;137(3):121-7.

Solubility Data

Solubility (In Vitro)	H2O :~100 mg/mL (~33.29 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 100 mg/mL (33.29 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.3329 mL	1.6643 mL	3.3286 mL
	5 mM	0.0666 mL	0.3329 mL	0.6657 mL
	10 mM	0.0333 mL	0.1664 mL	0.3329 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.