L-365260 hemihydrate

Name: L-365260 hemihydrate
Brand: MedChemExpress
SKU: HY-106840A
Rating: 5.0 (2 reviews)

製品番号: HY-106840A 純度: 99.75%: Data Sheet SDS COA 取扱説明書
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Technical Support

L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

L-365260 hemihydrate 構造式

容量	価格（税別）	在庫状況	数量
5 mg	$186	在庫あり	Estimated Time of Arrival: December 31
10 mg		お問い合わせ
50 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.

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Other Forms of L-365260 hemihydrate:

L-365260 在庫あり

顧客検証

Cholecystokinin Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

CCKAR CCKBR

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

製品説明

IC₅₀ & Target

Ki: 1.9 nM (gastrin); 2.0 nM (CCK-B)^[1].

体外実験

L-365260 hemihydrate exhibits a similar high affinity for brain CCK-B receptors of rats, mice and man, and a lower affinity for gastrin and brain CCK-B (IC₅₀=20-40 nM) receptors in dog tissues^[1].
L-365260 (1 μM) hemihydrate strongly attenuates the CCK8S- and CCK4-mediated depolarization in a different neuron^[2].

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

体内実験

L-365260 hemihydrate (0.1-30 mg/kg; p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED₅₀=0.03 mg/kg), rats (ED₅₀=0.9 mg/kg) and guinea pigs (ED₅₀=5.1 mg/kg)^[1].
L-365260 hemihydrate (0.01-10 mg/kg; s.c.) enhances analgesia induced by a submaximal dose of Morphine (4 mg/kg) in rats^[3].
L-365260 hemihydrate (0.2 mg/kg; s.c. twice daily for 5 days) significantly prolongs the duration of Morphine analgesia in rats^[3].

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

Animal Model:	Male Sprague-Dawley rats (300-350 g; Morphine- injected)^[3].
Dosage:	0.01, 0.05, 0.1, 0.2, 0.75, 1.0, 10.0 mg/kg
Administration:	S.c. 10 min prior to i.p. injection of 4 mg/kg Morphine
Result:	Enhanced morphine analgesia.

分子量

407.47

分子式

C₂₄H₂₄N₄O₃

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=CC(C)=C1)N[C@H]2C(N(C)C3=CC=CC=C3C(C4=CC=CC=C4)=N2)=O.[1/2].O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

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

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (122.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4542 mL	12.2708 mL	24.5417 mL
5 mM	0.4908 mL	2.4542 mL	4.9083 mL
10 mM	0.2454 mL	1.2271 mL	2.4542 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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）

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

純度とドキュメンテーション

純度: 99.75%

Select Batch:

データシート (280 KB) SDS (251 KB)

COA (258 KB) HNMR (261 KB) RP-HPLC (141 KB) LCMS (206 KB) Elemental Analysis Report (116 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Lotti VJ, et, al. A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260. Eur J Pharmacol. 1989 Mar 21;162(2):273-80. [Content Brief]

[2]. Dourish CT, et, al. The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat. Eur J Pharmacol. 1990 Jan 25;176(1):35-44. [Content Brief]

[3]. Lotti VJ, et, al. A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260. Eur J Pharmacol. 1989 Mar 21;162(2):273-80. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4542 mL	12.2708 mL	24.5417 mL	61.3542 mL
	5 mM	0.4908 mL	2.4542 mL	4.9083 mL	12.2708 mL
	10 mM	0.2454 mL	1.2271 mL	2.4542 mL	6.1354 mL
	15 mM	0.1636 mL	0.8181 mL	1.6361 mL	4.0903 mL
	20 mM	0.1227 mL	0.6135 mL	1.2271 mL	3.0677 mL
	25 mM	0.0982 mL	0.4908 mL	0.9817 mL	2.4542 mL
	30 mM	0.0818 mL	0.4090 mL	0.8181 mL	2.0451 mL
	40 mM	0.0614 mL	0.3068 mL	0.6135 mL	1.5339 mL
	50 mM	0.0491 mL	0.2454 mL	0.4908 mL	1.2271 mL
	60 mM	0.0409 mL	0.2045 mL	0.4090 mL	1.0226 mL
	80 mM	0.0307 mL	0.1534 mL	0.3068 mL	0.7669 mL
	100 mM	0.0245 mL	0.1227 mL	0.2454 mL	0.6135 mL