Carbetocin (Synonyms: カルベトシン)

Name: Carbetocin
Brand: MedChemExpress
SKU: HY-17573
Rating: 5.0 (2 reviews)

製品番号: HY-17573 純度: 99.91%: Data Sheet SDS COA 取扱説明書
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Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a K_i of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (K_i=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.

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カスタムペプチド

Carbetocin 構造式

CAS 番号 : 37025-55-1

容量	価格（税別）	在庫状況	数量
5 mg	$60	在庫あり	Estimated Time of Arrival: December 31
10 mg	$90	在庫あり	Estimated Time of Arrival: December 31
25 mg	$200	在庫あり	Estimated Time of Arrival: December 31
50 mg	$350	在庫あり	Estimated Time of Arrival: December 31
100 mg	$560	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 2 publication(s) in Google Scholar

Other Forms of Carbetocin:

Carbetocin acetate 在庫あり
Carbetocin-d₇ お問い合わせ

顧客検証

おすすめ

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•関連小分子:

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製品説明

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	0.7 1 Compound: 2	Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	0.01 1 Compound: Carbetocin	Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	[PMID: 30896946]
CHO-K1	EC₅₀	0.7 1 Compound: 2	Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	> 10000 1 Compound: 2	Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
CHO-K1	EC₅₀	0.7 1 Compound: 2	Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human oxytocin receptor expressed in CHO-K1 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	IC₅₀	> 10000 1 Compound: 2	Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	2.3 1 Compound: Carbetocin	Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	[PMID: 30896946]
HEK293	EC₅₀	0.01 1 Compound: Carbetocin	Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	[PMID: 30896946]
HEK293	EC₅₀	0.01 1 Compound: Carbetocin	Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method Agonist activity at recombinant human OTR expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	[PMID: 30896946]
HEK293	EC₅₀	4.8 1 Compound: Carbetocin	Agonist activity at recombinant human V1b receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method Agonist activity at recombinant human V1b receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	[PMID: 30896946]
HEK293	EC₅₀	170 1 Compound: 2	Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	170 1 Compound: 2	Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	>10 3 Compound: 2	Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	2.3 1 Compound: Carbetocin	Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	[PMID: 30896946]
HEK293	EC₅₀	2.3 1 Compound: Carbetocin	Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method Agonist activity at recombinant human V1a receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	[PMID: 30896946]
HEK293	IC₅₀	>10 3 Compound: 2	Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	4.8 1 Compound: Carbetocin	Agonist activity at recombinant human V1b receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method Agonist activity at recombinant human V1b receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	[PMID: 30896946]
HEK293	EC₅₀	4.8 1 Compound: Carbetocin	Agonist activity at recombinant human V1b receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method Agonist activity at recombinant human V1b receptor expressed in HEK293 cells assessed as increase in intracellular calcium level measured at 3 secs interval for 5 mins by fura-2/AM dye based micro spectrofluorometric method	[PMID: 30896946]
HEK293	EC₅₀	41 1 Compound: 2	Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	41 1 Compound: 2	Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	170 1 Compound: 2	Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	41 1 Compound: 2	Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	EC₅₀	> 10000 1 Compound: 2	Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]
HEK293	IC₅₀	> 10000 1 Compound: 2	Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay	[PMID: 24874785]

体外実験

Carbetocin is an agonist with about 10-fold lower affinity for the oxytocin receptor but with significantly higher stability and a longer duration of action. Carbetocin has higher affinity to the chimeric E1 receptor and especially to each of the combinations of E1 with the other extracellular domains, i.e. chimeric receptors E13 (K_i=13 nM), E123 (K_i=56 nM), and E1234 (K_i=37 nM)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Carbetocin (2-20 mg/kg; i.p.) has a significant effect of treatment on the percent time spent climbing, swimming and immobile^[1].
Carbetocin (1, 10,100 μg/rat, i.c.v.) reveals a dose-dependent increase in the percent time spent swimming and a corresponding reduction in immobility following acute administration of 100 μg/rat^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley rats weighing between 300 and 500 g^[1]
Dosage:	2, 6.4, 20 mg/kg
Administration:	IP; single dose
Result:	Increased climbing with 6.4 mg/kg and resulted in a significantly greater proportion of time spent swimming with 20 mg/kg.

臨床実験

分子量

988.16

分子式

C₄₅H₆₉N₁₁O₁₂S

CAS 番号

37025-55-1

Appearance

Solid

Color

White to off-white

Sequence

Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2

Sequence Shortening

CYIQNCPLG-NH2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

polypeptide, sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (polypeptide, sealed storage, away from moisture and light, under nitrogen)

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (101.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 33.33 mg/mL (33.73 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0120 mL	5.0599 mL	10.1198 mL
5 mM	0.2024 mL	1.0120 mL	2.0240 mL
10 mM	0.1012 mL	0.5060 mL	1.0120 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 99.97%

Select Batch:

データシート (283 KB) SDS (419 KB)

COA (260 KB) HNMR (320 KB) RP-HPLC (201 KB) MS (72 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Stella Chaviaras, et al. 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. [Content Brief]

[2]. Gerald Gimpl, et al. 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. [Content Brief]

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

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.0120 mL	5.0599 mL	10.1198 mL	25.2995 mL
	5 mM	0.2024 mL	1.0120 mL	2.0240 mL	5.0599 mL
	10 mM	0.1012 mL	0.5060 mL	1.0120 mL	2.5300 mL
	15 mM	0.0675 mL	0.3373 mL	0.6747 mL	1.6866 mL
	20 mM	0.0506 mL	0.2530 mL	0.5060 mL	1.2650 mL
	25 mM	0.0405 mL	0.2024 mL	0.4048 mL	1.0120 mL
	30 mM	0.0337 mL	0.1687 mL	0.3373 mL	0.8433 mL
DMSO	40 mM	0.0253 mL	0.1265 mL	0.2530 mL	0.6325 mL
	50 mM	0.0202 mL	0.1012 mL	0.2024 mL	0.5060 mL
	60 mM	0.0169 mL	0.0843 mL	0.1687 mL	0.4217 mL
	80 mM	0.0126 mL	0.0632 mL	0.1265 mL	0.3162 mL
	100 mM	0.0101 mL	0.0506 mL	0.1012 mL	0.2530 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Carbetocin Related Classifications

Neurological Disease Endocrinology

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Carbetocin37025-55-1Oxytocin ReceptorOXTRN-terminusE1postpartumhemorrhageantidepressant-likeblood-brainbarrierbbbInhibitorinhibitorinhibit

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Carbetocin (Synonyms: カルベトシン)

カスタマーレビュー

Other Forms of Carbetocin:

Carbetocin 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Carbetocin 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Carbetocin Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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