1. GPCR/G Protein
  2. Motilin Receptor
  3. MA-2029

MA-2029 

Cat. No.: HY-107642 Purity: >99.0%
Handling Instructions

MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=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.

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

MA-2029 Chemical Structure

MA-2029 Chemical Structure

CAS No. : 287206-61-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 704 In-stock
Estimated Time of Arrival: December 31
1 mg USD 190 In-stock
Estimated Time of Arrival: December 31
5 mg USD 575 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

MA-2029 is a selective, orally active, and competitive motilin receptor antagonist (IC50=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 pA2 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 [125I]motilin to motilin receptors in a homogenate of rabbit colon smooth muscle tissue and membranes of HEK 293 cells expressing human motilin receptors. The pKi of MA-2029 is 8.58±0.04 in the rabbit colon homogenate and 8.39 in the HEK 293 cells[1].

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 t1/2 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].

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 t1/2 is 2 hours.
Molecular Weight

556.71

Formula

C₃₁H₄₅FN₄O₄

CAS No.

287206-61-5

SMILES

FC(C=C1)=CC=C1C[[email protected]](NC)C(N(C)[[email protected]@H](C(C)C)C(N[[email protected]](C(NCC)=O)CC2=CC(C(C)(C)C)=C(O)C=C2)=O)=O

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

Purity: >99.0%

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Keywords:

MA-2029MA2029MA 2029Motilin ReceptorMLNRcontractionsgastrointestinalmotilityvisceralHEK 293cellsirritablebowelsyndromepKiselectiveInhibitorinhibitorinhibit

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MA-2029
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HY-107642
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