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S5701

SR 49059

Name: SR 49059
Brand: SIGMA

≥97% (HPLC), Arginine Vasopressin (AVP) V1a-receptor antagonist, powder

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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关于此项目

经验公式（希尔记法）:

C₂₈H₂₇Cl₂N₃O₇S

化学文摘社编号:

150375-75-0

分子量:

620.50

UNSPSC Code:

51111800

PubChem Substance ID:

329824460

NACRES:

NA.77

MDL number:

MFCD00922133

Assay:

≥97% (HPLC)

Form:

powder

Quality level:

100

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属性

产品名称

SR 49059, ≥97% (HPLC)

Quality Level

100

assay

≥97% (HPLC)

form

powder

optical activity

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

color

white to off-white

solubility

DMSO: ≥10 mg/mL

originator

Sanofi Aventis

storage temp.

2-8°C

SMILES string

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 key

CEBYCSRFKCEUSW-NAYZPBBASA-N

Gene Information

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

说明

Application

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。

Biochem/physiol Actions

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。

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。

Features and Benefits

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。

存储类别

11 - Combustible Solids

wgk

nwg

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

新产品

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

026M4758V

052M4613V

040M4607

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cAMP/PKA-dependent increases in Ca Sparks, oscillations and SR Ca stores in retinal arteriolar myocytes after exposure to vasopressin.

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

The effect of relcovaptan (SR 49059), an orally active vasopressin V1a receptor antagonist, on uterine contractions in preterm labor.

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

Evidence for a role of vasopressin in the control of aldosterone secretion in primary aldosteronism: in vitro and in vivo studies.

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

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