Chlorpropamide

製品コードS4166 バッチS416601

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₀H₁₃ClN₂O₃S
	分子量	276.74	CAS No.	94-20-2
Solubility (25°C)*	体外	DMSO	55 mg/mL (198.74 mM)
		Ethanol	55 mg/mL (198.74 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Chlorpropamide inhibits Na(+),K(+)-ATPase and stimulates a high affinity cyclic AMP-phosphodiesterase of isolated liver plasma membrane. Chlorpropamide is a sulfonylurea class drug for type 2 diabetes mellitus.
in vitro	Chlorpropamide acts through a cyclic AMP-independent mechanism. The addition of 0.2 mM Chlorpropamide to hepatocytes isolated from fed rats, raises the cellular concentration of fructose-2,6-bisphosphate (F-2, 6-P₂). The accumulation of F-2, 6-P₂ caused by Chlorpropamide (1 mM) is parallel to the stimulation of L-lactate production (36.6 versus 26.1 μmol of lactate/g of cells) and to the inhibition of gluconeogenesis (0.57 versus 0.94 μmol of [U-¹⁴C]pyruvate converted to glucose/g of cells). Chlorpropamide enhances the inhibitory action evoked by insulin on glucagon-stimulated gluconeogenesis^[1]. Chlorpropamide treatment has no effect on insulin binding, altering neither receptor number nor affinity in rat adipocytes. Chlorpropamide (175 μg/mL) enhances 2-deoxyglucose transport in both the absence (17%) and presence (20%) of insulin. Chlorpropamide significantly increases glucose metabolism and total lipids in both the absence (30%) and presence (31%) of insulin^[2]. Chlorpropamide competitively inhibits antidiuretic hormone (ADH) binding and adenylyl cyclase (AC) stimulation with K_i of 2.8 mM and 250 μM, respectively, in the LLC-PK1 cell line. Chlorpropamide (333 μM) increases the apparent K_a of ADH for AC activation (0.31 vs. 0.08 nM) without affecting a maximal response. Twenty-four-hour Chlorpropamide exposure (100 μM) upregulates the ADH receptors without affecting affinity, which lowers K_a and increases basal AC activity and maximal response (1.86 vs. 1.35 and 14.9 vs. 10.6 fmol cAMP/min/1000 cells).

製品説明

Chlorpropamide inhibits Na(+),K(+)-ATPase and stimulates a high affinity cyclic AMP-phosphodiesterase of isolated liver plasma membrane. Chlorpropamide is a sulfonylurea class drug for type 2 diabetes mellitus.

in vitro

Chlorpropamide acts through a cyclic AMP-independent mechanism. The addition of 0.2 mM Chlorpropamide to hepatocytes isolated from fed rats, raises the cellular concentration of fructose-2,6-bisphosphate (F-2, 6-P₂). The accumulation of F-2, 6-P₂ caused by Chlorpropamide (1 mM) is parallel to the stimulation of L-lactate production (36.6 versus 26.1 μmol of lactate/g of cells) and to the inhibition of gluconeogenesis (0.57 versus 0.94 μmol of [U-¹⁴C]pyruvate converted to glucose/g of cells). Chlorpropamide enhances the inhibitory action evoked by insulin on glucagon-stimulated gluconeogenesis^[1]. Chlorpropamide treatment has no effect on insulin binding, altering neither receptor number nor affinity in rat adipocytes. Chlorpropamide (175 μg/mL) enhances 2-deoxyglucose transport in both the absence (17%) and presence (20%) of insulin. Chlorpropamide significantly increases glucose metabolism and total lipids in both the absence (30%) and presence (31%) of insulin^[2]. Chlorpropamide competitively inhibits antidiuretic hormone (ADH) binding and adenylyl cyclase (AC) stimulation with K_i of 2.8 mM and 250 μM, respectively, in the LLC-PK1 cell line. Chlorpropamide (333 μM) increases the apparent K_a of ADH for AC activation (0.31 vs. 0.08 nM) without affecting a maximal response. Twenty-four-hour Chlorpropamide exposure (100 μM) upregulates the ADH receptors without affecting affinity, which lowers K_a and increases basal AC activity and maximal response (1.86 vs. 1.35 and 14.9 vs. 10.6 fmol cAMP/min/1000 cells).

プロトコル(参考用のみ)

参考

[4] P Luly, et al. Eur J Pharmacol. 1977 Nov 15;46(2):153-64.

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A network integration approach for drug-target interaction prediction and computational drug repositioning from heterogeneous information. [ Nat Commun, 2017, 8(1):573]	PubMed: 28924171

A network integration approach for drug-target interaction prediction and computational drug repositioning from heterogeneous information. [ Nat Commun, 2017, 8(1):573]

PubMed: 28924171

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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