卡贝缩宫素是一种激动剂，对催产素受体的亲和力大约低 10 倍，但稳定性明显更高，作用持续时间更长。卡贝缩宫素对嵌合 E1 受体，尤其是 E1 与其他胞外结构域的每种组合，即嵌合受体 E13 (Ki=13 nM)、E123 (Ki=56 nM) 和 E1234 (Ki=37 nM) 具有较高的亲和力。 ）[2]。

卡贝缩宫素（2-20 mg/kg；腹膜内注射）对攀爬、游泳和不动的时间百分比有显着影响[1]。卡贝缩宫素（1, 10,100 μg/大鼠，icv）显示，急性给药 100 μg/大鼠后，游泳时间百分比呈剂量依赖性增加，而不动性相应减少[1]。动物模型：雄性 Sprague-Dawley 大鼠，体重 300 至 500 g[1] 剂量：2、6.4、20 mg/kg 给药方式：IP；单剂量结果：6.4 mg/kg 增加攀爬时间，20 mg/kg 则显着增加游泳时间。

Male Sprague-Dawley rats weighing between 300 and 500 g
2, 6.4, 20 mg/kg
IP; single dose

Absorption, Distribution and Excretion
Bioavailability is 80% following intramuscular injection.

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Biological Half-Life
40 minutes

[1]. Assessing the antidepressant-like effects of carbetocin, an oxytocin agonist, using a modification of the forced swimming test. Psychopharmacology (Berl). 2010 May;210(1):35-43.

[2]. Binding domains of the oxytocin receptor for the selective oxytocin receptor antagonist barusiban in comparison to the agonists oxytocin and carbetocin. Eur J Pharmacol. 2005 Mar 7;510(1-2):9-16.

[3]. The effects of oxytocin and its analog, carbetocin, on genetic deficits in sensorimotor gating. Eur Neuropsychopharmacol. 2012 May;22(5):374-8.

Carbetocin is oxytocin in which the hydrogen on the phenolic hydroxy group is substituted by methyl, the amino group on the cysteine residue is substituted by hydrogen, and the sulfur of the cysteine residue is replaced by a methylene group. A synthetic carba-analogue of oxytocin, it is used to control bleeding after giving birth. Like oxytocin, it causes contraction of the uterus. It has a role as an oxytocic.
Carbetocin is a drug used to control postpartum hemorrhage, bleeding after giving birth. It is an analogue of oxytocin, and its action is similar to that of oxytocin -- it causes contraction of the uterus.
Carbetocin is a long-acting synthetic agonist analogue of human oxytocin, with antihemorrhagic and uterotonic activities. Upon administration, carbetocin targets, binds to and activates peripheral oxytocin receptors that are present on the smooth musculature of the uterus. This causes uterus contractions and prevents excessive bleeding after childbirth, particularly following Cesarean section, and may be used to decrease blood loss during hysteroscopic myomectomy.

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Drug Indication
Used to control postpartum hemorrhage and bleeding after giving birth.

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Mechanism of Action
Carbetocin binds to oxytocin receptors present on the smooth musculature of the uterus, resulting in rhythmic contractions of the uterus, increased frequency of existing contractions, and increased uterine tone. The oxytocin receptor content of the uterus is very low in the non-pregnant state, and increases during pregnancy, reaching a peak at the time of delivery.

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Pharmacodynamics
Carbetocin is a drug used to control postpartum hemorrhage, bleeding after giving birth. It is sold under the trade name Duratocin. It is an analogue of oxytocin, and its action is similar to that of oxytocin; it causes contraction of the uterus.

C45H69N11O12S

988.170

987.484

C, 54.70; H, 7.04; N, 15.59; O, 19.43; S, 3.24

37025-55-1

Carbetocin acetate; 1631754-28-3

16681432

White to off-white solid powder

1.2±0.1 g/cm3

1477.9±65.0 °C at 760 mmHg

847.6±34.3 °C

0.0±0.3 mmHg at 25°C

1.533

-3.59

387.81

10

13

18

69

1850

8

O=C([C@H](CSCCCC(N[C@H](C1=O)CC2=CC=C(OC)C=C2)=O)NC([C@@H](NC([C@](NC([C@](N1)([H])[C@@H](C)CC)=O)([H])CCC(N)=O)=O)CC(N)=O)=O)N(CCC3)[C@@H]3C(N[C@@H](CC(C)C)C(NCC(N)=O)=O)=O

NSTRIRCPWQHTIA-DTRKZRJBSA-N

InChI=1S/C45H69N11O12S/c1-6-25(4)38-44(66)51-28(15-16-34(46)57)40(62)52-31(21-35(47)58)41(63)54-32(23-69-18-8-10-37(60)50-30(42(64)55-38)20-26-11-13-27(68-5)14-12-26)45(67)56-17-7-9-33(56)43(65)53-29(19-24(2)3)39(61)49-22-36(48)59/h11-14,24-25,28-33,38H,6-10,15-23H2,1-5H3,(H2,46,57)(H2,47,58)(H2,48,59)(H,49,61)(H,50,60)(H,51,66)(H,52,62)(H,53,65)(H,54,63)(H,55,64)/t25-,28-,29-,30-,31-,32-,33-,38-/m0/s1

(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]-1-[(3R,6S,9S,12S,15S)-6-(2-amino-2-oxoethyl)-9-(3-amino-3-oxopropyl)-12-[(2S)-butan-2-yl]-15-[(4-methoxyphenyl)methyl]-5,8,11,14,17-pentaoxo-1-thia-4,7,10,13,16-pentazacycloicosane-3-carbonyl]pyrrolidine-2-carboxamide

EINECS-253-312-6; EINECS 253-312-6; Carbetocin; EINECS253-312-6

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O: ≥ 33.3 mg/mL (~33.7 mM)
DMSO: ≥ 31 mg/mL (~31.4 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (2.53 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (2.53 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (2.53 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。