MRS 1706
MRS 1706 Basic information
- Product Name:
- MRS 1706
- Synonyms:
-
- MRS-1706;MRS 1706;MRS1706
- N-(4-ACETYLPHENYL)-2-[4-(2,3,6,7-TETRAHYDRO-2,6-DIOXO-1,3-DIPROPYL-1H-PURIN-8-YL)PHENOXY]ACETAMIDE
- MRS 1706
- N-(4-acetylphenyl)-2-[4-(2,6-dioxo-1,3-dipropyl-7H-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]-
- N-(4-Acetylphenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,9-tetrahydro-1H-purin-8-yl)phenoxy)acetamide
- MRS-1706,cAMP,P1 receptor,corpus cavernosal strips,duration,inhibit,MRS 1706,Adenosine Receptor,MRS1706,Inhibitor,adenosine,magnitude
- MRS-1706, 10 mM in DMSO
- CAS:
- 264622-53-9
- MF:
- C27H29N5O5
- MW:
- 503.55
- Mol File:
- 264622-53-9.mol
MRS 1706 Chemical Properties
- 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
MRS 1706 Usage And Synthesis
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. |
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
MRS 1706Supplier
- Tel
- 821-50328103-801 18930552037
- 3bsc@sina.com
- Tel
- 888-539-0666
- info@emmx.com
- Tel
- 021-61312847; 18021002903
- 3008007409@qq.com
- Tel
- 13761635123
- 1014988033@qq.com
- Tel
- 025-58859352 18068836627
- dt3@aikonchem.com