[CAS NO. 287206-61-5] MA-2029
PRODUCTS SPECIFICATIONS [287206-61-5]
DESCRIPTION [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 |
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 |