[CAS NO. 287206-61-5] MA-2029

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Catalog:	HY-107642
Brand:	MCE
CAS:	287206-61-5

Overview

MDL	-
Molecular Weight	556.71
Molecular Formula	C31H45FN4O4
SMILES	FC(C=C1)=CC=C1C[C@H](NC)C(N(C)[C@@H](C(C)C)C(N[C@H](C(NCC)=O)CC2=CC(C(C)(C)C)=C(O)C=C2)=O)=O

For research use only. We do not sell to patients.

Summary

MA-2029 is a selective, orally active, and competitive motilin receptor antagonist ( IC ₅₀ =4.9 nM). MA-2029 is selective for the motilin receptor over various other receptors and ion channels. MA-2029 may be useful for gastrointestinal disorders associated with disturbed gastrointestinal motility ^[1] .

IC50 & Target

IC50: 4.9 nM (motilin receptor) ^[1]

In Vitro

MA-2029 (1 to 30 nM) competitively inhibits motilin-induced contractions in isolated rabbit duodenal longitudinal muscle strips, with a pA ₂ value of 9.17±0.01. Contractile responses to acetylcholine and substance P are unaffected even at 1 μM of MA-2029. MA-2029 concentration-dependently inhibits the binding of [ ¹²⁵ I]motilin to motilin receptors in a homogenate of rabbit colon smooth muscle tissue and membranes of HEK 293 cells expressing human motilin receptors. The pK _i of MA-2029 is 8.58±0.04 in the rabbit colon homogenate and 8.39 in the HEK 293 cells ^[1] .

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

In Vivo

MA-2029 (0.3-3 mg/kg; p.o.) dose-dependently inhibits the number of abdominal muscle contractions induced under the same conditions and causes significant inhibition at 3 mg/kg ^[1] .
MA-2029 (10 mg/kg; p.o.) treatment shows that the t _1/2 is 2 hours ^[1] .
The inhibition is significant at 30 min after administration of 3 mg/kg or more and at 4 h after administration of 10 mg/kg or more (MA-2029), so administration of 10 mg/kg or more causes inhibitory effects from 30 min or less to at least 4 h after administration ^[1] .

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

Animal Model:	Male Japanese-white rabbits (about 2-3 kg) ^[1]
Dosage:	0.3, 1, 3 mg/kg
Administration:	Oral administration
Result:	Dose-dependently inhibited the number of abdominal muscle contractions induced under the same conditions. Caused significant inhibition at 3 mg/kg.

Animal Model:	Male Japanese-white rabbits (about 2-3 kg) ^[1]
Dosage:	10 mg/kg
Administration:	Oral administration (Pharmacokinetic Analysis)
Result:	The t _1/2 is 2 hours.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

References

[1] Sudo H, et al. Oral administration of MA-2029, a novel selective and competitive motilin receptor antagonist, inhibits motilin-induced intestinal contractions and visceral pain in rabbits. Eur J Pharmacol. 2008 Mar 10;581(3):296-305.

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