| Identification | Back Directory | [Name]
MRS 1706 | [CAS]
264622-53-9 | [Synonyms]
MRS 1706
MRS-1706;MRS 1706;MRS1706
N-(4-acetylphenyl)-2-[4-(2,6-dioxo-1,3-dipropyl-7H-purin-8-yl)phenoxy]acetamide
N-(4-ACETYLPHENYL)-2-[4-(2,3,6,7-TETRAHYDRO-2,6-DIOXO-1,3-DIPROPYL-1H-PURIN-8-YL)PHENOXY]ACETAMIDE
N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide
Acetamide, N-(4-acetylphenyl)-2-[4-(2,3,6,9-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)phenoxy]- | [Molecular Formula]
C27H29N5O5 | [MDL Number]
MFCD28160689 | [MOL File]
264622-53-9.mol | [Molecular Weight]
503.55 |
| Chemical Properties | Back Directory | [density ]
1.293±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO : 6.4 mg/mL (12.71 mM; Need ultrasonic and warming)H2O : < 0.1 mg/mL (insoluble) | [form ]
Powder | [pka]
8.25±0.70(Predicted) | [color ]
Off-white to yellow | [InChIKey]
ZKUCFFYOQOJLGT-UHFFFAOYSA-N | [SMILES]
O=C(COC1=CC=C(C=C1)C2=NC3=C(N2)N(C(N(C3=O)CCC)=O)CCC)NC4=CC=C(C=C4)C(C)=O |
| Hazard Information | Back Directory | [Description]
MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively. | [Uses]
MRS 1706 is a selective and potent Adenosine A2B-R inverse agonist Ki (binding affinity) values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively. | [Biological Activity]
Potent and selective adenosine A 2B receptor inverse agonist (K i values are 1.39, 157, 112 and 230 nM for human A 2B , A 1 , A 2A and A 3 receptors respectively). | [in vivo]
MRS-1706 (1-10 μM; intracavernous injection; Ada–/– mice) reduces the magnitude and duration of electrical field stimulation (EFS)-induced contraction of corpus cavernosal strips (CCSs) from sickle cell disease (SCD) transgenic mice and inhibits the level of cAMP[2]. | Animal Model: | Ada–/– mice[2] | | Dosage: | 1 and 10 μM | | Administration: | Intracavernous injection | | Result: | Inhibited A2BR signaling and reduced the magnitude and duration.
Inhibited the level of cAMP.
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| [References]
[1] YONG-CHUL KIM. Anilide Derivatives of an 8-Phenylxanthine Carboxylic Congener Are Highly Potent and Selective Antagonists at Human A2B Adenosine Receptors[J]. Journal of Medicinal Chemistry, 2000, 43 6: 1165-1172. DOI: 10.1021/jm990421v
[2] QILAN LI. ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 320 2: 637-645. DOI: 10.1124/jpet.106.111203 |
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| Company Name: |
cjbscvictory
|
| Telephone: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
| Company Name: |
Bide Pharmatech Ltd.
|
| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
|