AC 187 TFA
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 3004.27 |
| Molecular Formula | C129H206F3N37O42 |
| SMILES | - |
Summary
AC 187 TFA is a potent and orally active amylin receptor antagonist with an IC 50 of 0.48 nM and a K i of 0.275 nM. AC 187 TFA shows more selective for amylin receptor than calcitonin and CGRP receptors. AC 187 TFA has neuroprotective effects [1] [2] .
IC50 & Target
IC50: 0.48 nM (amylin receptor)
In Vitro
AC 187 blocks amyloidβ protein (Aβ)-induced neurotoxicity. Treatment of cultures with AC 187 before exposure to Aβ results in significantly improved neuronal survival
[1]
.
AC187 attenuates the activation of initiator and effector caspases that mediate Aβ-induced apoptotic cell death
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AC 187 (30 mg/mL) increases glucagon concentration, accelerates gastric emptying of liquids, and results in an exaggerated post-challenge glycemia in hyperinsulinemic clamps in Sprague-Dawley (HSD) rats [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 33.29 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (33.29 mM); Clear solution; Need ultrasonic
References
- [1] Jack H Jhamandas, et al. 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] Bronislava R Gedulin, et al. 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.