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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
MA-2029 targets the motilin receptor. It acts as a selective, competitive antagonist with an IC50 of 4.9 nM. The compound has a pA2 value of 9.17 and shows high selectivity over a range of other receptors and ion channels.
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| ln Vitro |
The contraction of isolated rabbit duodenum longitudinal muscle strips elicited by motilin is competitively inhibited by MA-2029 (1 to 30 nM), showing a pA2 value of 9.17˱0.01. Even at a dosage of 1 μM MA-2029, contractile responses to substance P and acetylcholine remained unaltered. Rabbit colonic smooth muscle tissue and HEK 293 cell membrane homogenates expressing human motilin receptors are subject to concentration-dependent inhibition of [125I]motilin binding by MA-2029. pKi for MA-2029 is 8.38 in HEK 293 cells and 8.58±0.04 in rabbit colon homogenate [1].
MA-2029 potently inhibits the motilin receptor with an IC50 of 4.9 nM and displaces [125I]motilin with an IC50 of 2.74 nM. It shows high selectivity over other receptors and ion channels. The compound inhibits motilin-induced intestinal contractions and visceral pain in rabbits. |
| ln Vivo |
The number of abdominal muscular contractions elicited under the same conditions is dosage-dependently inhibited by MA-2029 (0.3-3 mg/kg; oral), with a dose of 3 mg/kg causing a considerable suppression [1]. The oral MA-2029 (10 mg/kg) therapy showed a t1/2 of two hours [1]. When 3 mg/kg or more is administered, significant inhibition happens 30 minutes later, and when 10 mg/kg or more is administered, it happens 4 hours later (MA-2029). As a result, the inhibitory action starts to take effect 30 minutes after administering 10 mg/kg or greater, or at least 4 hours later [ 1].
In vivo, MA-2029 is orally active and inhibits motilin-induced intestinal contractions and visceral pain in rabbits. The compound has potential applications in gastrointestinal disorders associated with disturbed gastrointestinal motility. Its oral activity makes it suitable for therapeutic development. |
| Enzyme Assay |
In vitro receptor binding assays measure the displacement of [125I]motilin from motilin receptors expressed in cell membranes. MA-2029 is incubated with membrane preparations and the radiolabeled ligand, and the IC50 is determined. Functional assays measure the inhibition of motilin-induced contractions in smooth muscle preparations.
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| Cell Assay |
In vitro cellular assays evaluate the antagonist activity of MA-2029 on cells expressing the motilin receptor. Cells are treated with motilin in the presence or absence of MA-2029, and receptor activation is measured by calcium mobilization or other second messenger assays. The IC50 for antagonism is determined from dose-response curves.
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| Animal Protocol |
Animal/Disease Models: Male Japanese white rabbit (approximately 2-3 kg) [1]
Doses: 0.3, 1, 3 mg/kg Route of Administration: Oral Experimental Results:Dose-dependent inhibition of the number of abdominal muscle contractions induced under the same conditions. 3 mg/kg caused significant inhibition. Animal/Disease Models: Male Japanese white rabbit (approximately 2-3 kg) [1] Doses: 10 mg/kg Route of Administration: Oral (pharmacokinetic/PK/PK analysis) Experimental Results: t1/2 is 2 hrs (hrs (hours)). In vivo animal experiments are conducted in rabbit models to study the effects of MA-2029 on gastrointestinal motility. The compound is administered orally or intravenously. Motilin-induced intestinal contractions and visceral pain are measured. The compound's effects on gastrointestinal motility are assessed. |
| ADME/Pharmacokinetics |
MA-2029 has a CAS number of 287206-61-5. It is an orally active, competitive motilin receptor antagonist. The compound is also known as MA 2029 and MA2029. Its chemical name is 4-Fluoro-N-methyl-L-phenylalanyl-N-methyl-L-valyl-3-(1,1-dimethylethyl)-N-ethyl-L-tyrosinamide.
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| Toxicity/Toxicokinetics |
The toxicity profile of MA-2029 is related to its mechanism as a motilin receptor antagonist. The compound shows high selectivity over other receptors and ion channels, suggesting a favorable safety profile. Standard toxicological studies would be required for clinical development.
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| References | |
| Additional Infomation |
See also: MA-2029 (notes moved to).
MA-2029 is a research tool for studying the role of motilin in gastrointestinal motility. It has potential therapeutic applications in gastrointestinal disorders associated with disturbed motility. The compound is also known as a selective motilin receptor antagonist. It has been used to study the physiological and pathological roles of motilin signaling. |
| Molecular Formula |
C31H46CLFN4O4
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|---|---|
| Molecular Weight |
593.17275094986
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| Exact Mass |
556.342
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| CAS # |
287206-61-5
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| PubChem CID |
10144175
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| Appearance |
White to off-white solid powder
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
40
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| Complexity |
825
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| Defined Atom Stereocenter Count |
3
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| SMILES |
Cl.CCNC([C@H](CC1C=CC(O)=C(C(C)(C)C)C=1)NC([C@@H](N(C([C@H](CC1=CC=C(F)C=C1)NC)=O)C)C(C)C)=O)=O
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| InChi Key |
KSDWAJPUTRBIRR-KLJDGLGGSA-N
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| InChi Code |
InChI=1S/C31H45FN4O4/c1-9-34-28(38)24(18-21-12-15-26(37)23(16-21)31(4,5)6)35-29(39)27(19(2)3)36(8)30(40)25(33-7)17-20-10-13-22(32)14-11-20/h10-16,19,24-25,27,33,37H,9,17-18H2,1-8H3,(H,34,38)(H,35,39)/t24-,25-,27-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-3-(3-tert-butyl-4-hydroxyphenyl)-1-(ethylamino)-1-oxopropan-2-yl]-2-[[(2S)-3-(4-fluorophenyl)-2-(methylamino)propanoyl]-methylamino]-3-methylbutanamide
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| Synonyms |
MA2029; MA 2029; MA-2029
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6859 mL | 8.4293 mL | 16.8586 mL | |
| 5 mM | 0.3372 mL | 1.6859 mL | 3.3717 mL | |
| 10 mM | 0.1686 mL | 0.8429 mL | 1.6859 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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