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S5701

Sigma-Aldrich

SR 49059

≥97% (HPLC)

别名:

(2S)-1-[[(2r,3s)-5-氯-3-(2-氯苯基)-1-[(3,4-二甲氧基苯基)磺酰基]-2,3-二氢-3-羟基-1H-吲哚-2-基]羰基]-2-吡咯烷羧酰胺, SR49059

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About This Item

经验公式（希尔记法）:
C28H27Cl2N3O7S
CAS号:
150375-75-0
分子量:
620.50
MDL號碼:
MFCD00922133
分類程式碼代碼:
51111800
PubChem物質ID:
329824460
NACRES:
NA.77

品質等級

100

化驗

≥97% (HPLC)

形狀

powder

光學活性

[α]/D -180 to -190°, c = 0.3 in chloroform-d

顏色

white to off-white

溶解度

DMSO: ≥10 mg/mL

起源

Sanofi Aventis

儲存溫度

2-8°C

SMILES 字串

COc1ccc(cc1OC)S(=O)(=O)N2[C@@H](C(=O)N3CCC[C@H]3C(N)=O)[C@@](O)(c4ccccc4Cl)c5cc(Cl)ccc25

InChI

1S/C28H27Cl2N3O7S/c1-39-23-12-10-17(15-24(23)40-2)41(37,38)33-21-11-9-16(29)14-19(21)28(36,18-6-3-4-7-20(18)30)25(33)27(35)32-13-5-8-22(32)26(31)34/h3-4,6-7,9-12,14-15,22,25,36H,5,8,13H2,1-2H3,(H2,31,34)/t22-,25-,28+/m0/s1

InChI 密鑰

CEBYCSRFKCEUSW-NAYZPBBASA-N

基因資訊

human ... AVPR1A(552) , OXTR(5021)

應用

SR 49059可用于精氨酸加压素（AVP）V1a受体介导的细胞信号转导研究中。
SR 49059已用于研究V1AR（1A型加压素受体）信号传导介导的 β肾上腺素能受体反应性及其对心力衰竭发展的影响。

生化／生理作用

SR 49059是一种有效的选择性精氨酸后叶加压素(AVP) V1a-受体拮抗剂。AVP是一种激素，在循环和水的稳态中发挥重要作用，并且在充血性心力衰竭（CHF）中对肾脏血流动力学改变、保水力和心脏重塑等具有重要作用。AVP受体有三种亚型，即V1a、V1b和V2。它们均属于大型视紫红质样G蛋白偶联受体家族。V(1a)拮抗剂可改善CHF中的水平衡和心脏肥大，可能有益于CHF中的保水力和心脏重塑。SR 49059在治疗雷诺氏病、痛经和安胎方面也显示出初步的积极结果。

特點和優勢

该化合物由Sanofi Aventis开发。要浏览其他药物开发化合物和批准的药物/候选药物列表，单击此处。

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

nwg

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析证书(COA)

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Margareta Steinwall et al.
Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology, 20(2), 104-109 (2005-04-13)
Relcovaptan (SR 49059) is a non-peptide, orally active vasopressin V1a receptor inhibitor. The effect on uterine contractions in 18 women with preterm labor in pregnancy weeks 32-36 was assessed in a double-blind investigation. The inclusion criterion was at least four
Owen Jeffries et al.
Investigative ophthalmology & visual science, 51(3), 1591-1598 (2009-12-05)
To investigate the effects of arginine vasopressin (AVP) on Ca(2+) sparks and oscillations and on sarcoplasmic reticulum (SR) Ca(2+) content in retinal arteriolar myocytes. Fluo-4-loaded smooth muscle in intact segments of freshly isolated porcine retinal arteriole was imaged by confocal
Véronique Perraudin et al.
The Journal of clinical endocrinology and metabolism, 91(4), 1566-1572 (2006-02-02)
Arginine vasopressin (AVP) stimulates steroid secretion from the normal human adrenal gland and some cortisol-producing adrenocortical tumors or hyperplasia through activation of the V(1a) receptor. The objective of the study was to investigate in vitro and in vivo the possible
Junko Tsukada et al.
Vascular pharmacology, 42(2), 47-55 (2005-02-22)
The pharmacologic profile of YM218, (Z)-4'-{4,4-difluoro-5-[2-oxo-2-(4-piperidinopiperidino)ethylidene]-2,3,4,5-tetrahydro-1H-1-benzoazepine-1-carbonyl}-2-methyl-3-furanilide hemifumarate, a newly synthesized, nonpeptide vasopressin (AVP) receptor antagonist, was investigated using several in vitro and in vivo methods. YM218 exhibited high affinity for V1A receptors isolated from rat liver, with a Ki value
Virginie Bernier et al.
Journal of the American Society of Nephrology : JASN, 17(1), 232-243 (2005-12-02)
In many mendelian diseases, some mutations result in the synthesis of misfolded proteins that cannot reach a transport-competent conformation. In X-linked nephrogenic diabetes insipidus, most of the mutant vasopressin 2 (V2) receptors are trapped in the endoplasmic reticulum and degraded.
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