RS 127445 HCl (Synonyms: RS-127445; MT 500; RS127445) |
カタログ番号GC10670 |
5-HT2B受容体拮抗剤、高親和性
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
RS-127445は、選択的で高親和性の5-HT2B受容体拮抗剤です。
5-HT2B受容体はGタンパク質共役受容体です。5-HT2B受容体は、さまざまな種の周辺組織で広く発現しています。 5-HT2B受容体は、胃ファンダスの平滑筋、食道、大腸、小腸を含む消化管全体に発現します。この受容体はまた、胎盤、子宮、肺および前立腺でも見つかっています。 5-HT2B受容体は多くの血管ベッドに存在し、血管平滑筋と血管内皮細胞の両方に局在していることが報告されています[1]。
RS-127445(2-アミノ-4-(4-フルオロナフト-1-イル)-6-イソプロピルピリミジン)は、5-HT2B受容体に対してpKiが9.5±0.1のナノモーラル親和性を示しました。人間の再構成5-HT2B受容体を発現する細胞では、RS-127445は強力にinositolリン酸の形成(pKB = 9.5 ± 0.1)および細胞内カルシウムの増加(pIC50 = 10.4 ± 0.1)を誘導する5-HTに拮抗作用を示しました。 RS-127445は、ラット孤立した胃底部の収縮(pA2 = 9.5 ± 1.1)および(±)α-methyl-5-HT介在下でラット頚静脈の弛緩(pA2 = 9.9 ± 0 .3)。ラットでは、RS-127445は経口または腹腔内投与経路から生物学的利用能がありました。
Reference:
[1] Bonhaus D W, Flippin L A, Greenhouse R J, et al. RS‐127445: a selective, high affinity, orally bioavailable 5‐HT2B receptor antagonist[J]. British journal of pharmacology, 1999, 127(5): 1075-1082.
Cas No. | N/A | SDF | |
同義語 | RS-127445; MT 500; RS127445 | ||
Chemical Name | 4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine hydrochloride | ||
Canonical SMILES | FC1=CC=C(C2=CC(C(C)C)=NC(N)=N2)C3=CC=CC=C31.Cl | ||
Formula | C17H17ClFN3 | M.Wt | 317.79 |
溶解度 | ≥ 31.8mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.1467 mL | 15.7337 mL | 31.4673 mL |
5 mM | 0.6293 mL | 3.1467 mL | 6.2935 mL |
10 mM | 0.3147 mL | 1.5734 mL | 3.1467 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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