(±)-U-50488 (Synonyms: (±)-trans-(1R,2R)-U-50488)

製品番号: HY-130696A: Data Sheet 取扱説明書
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(±)-U-50488 ((±)-trans-(1R,2R)-U-50488) is a selective kappa opioid receptor agonist. (±)-U-50488 can improve symptoms related to status epilepticus, but has no significant effect on spontaneous seizure episodes. (±)-U-50488 can be used for research of epilepsy.

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(±)-U-50488 構造式

CAS 番号 : 67198-13-4

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MOQ		Minimum order quantity
50 mg		お問い合わせ
100 mg		お問い合わせ
250 mg		お問い合わせ
Other size		お問い合わせ

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Other Forms of (±)-U-50488:

(+)-U-50488 お問い合わせ

Opioid 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

μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

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製品説明

IC₅₀ & Target^[1]

κ Opioid Receptor/KOR

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.3 1 Compound: U50488	Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay	[PMID: 25087049]
HEK-293T	IC₅₀	0.3 1 Compound: U50488	Agonist activity at recombinant human KOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay Agonist activity at recombinant human KOR expressed in HEK293T cells assessed as inhibition of forskolin-stimulated cAMP level preincubated for 15 to 20 mins followed by forskolin addition by GloSensor assay	[PMID: 28726402]
HEK293	IC₅₀	0.9 1 Compound: U-50488	Agonist activity at human KOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay Agonist activity at human KOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay	[PMID: 27776274]
CHO	EC₅₀	1.4 1 Compound: U-50488H	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	[PMID: 17981041]
CHO	EC₅₀	1.8 1 Compound: U50,488H	Agonist activity at human KOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting Agonist activity at human KOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting	[PMID: 31738550]
C6	IC₅₀	1.99 1 Compound: U-50488H	Displacement of [3H]dynorphin from human kappa opioid receptor expressed in C6 giloma cells Displacement of [3H]dynorphin from human kappa opioid receptor expressed in C6 giloma cells	[PMID: 19640720]
CHO	IC₅₀	6.4 × 10^-10 41 Compound: U-50488	Displacement of [3H]U 69593 from human recombinant kappa-opioid receptor expressed in CHO cells measured after 60 mins by scintillation counting method Displacement of [3H]U 69593 from human recombinant kappa-opioid receptor expressed in CHO cells measured after 60 mins by scintillation counting method	[PMID: 27876250]
CHO	IC₅₀	6.4 × 10^-10 41 Compound: U 50488	Displacement of [3H]U 69593 from rat recombinant kappa-type opioid receptor expressed in CHO cells Displacement of [3H]U 69593 from rat recombinant kappa-type opioid receptor expressed in CHO cells	[PMID: 26988801]
CHO	EC₅₀	2.9 1 Compound: U-50488H	Agonist activity at human KOPR expressed in CHO cells assessed as enhancement of [35S]GTPgammaS binding Agonist activity at human KOPR expressed in CHO cells assessed as enhancement of [35S]GTPgammaS binding	[PMID: 19147366]
CHO	EC₅₀	3.4 1 Compound: U-50488H	Binding potency at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Binding potency at human kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 16945525]
CHO	EC₅₀	3.4 1 Compound: U-50488H	Concentration required to enhance [35S]GTP-gamma-S, binding to human Opioid receptor kappa expressed in CHO cells Concentration required to enhance [35S]GTP-gamma-S, binding to human Opioid receptor kappa expressed in CHO cells	[PMID: 16051487]
CHO	EC₅₀	4.2 1 Compound: U50488	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [33S]GTPgammaS binding after 60 mins by scintillation counting	[PMID: 22439881]
CHO	EC₅₀	4.5 1 Compound: U-50488H	Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells Enhancement of [35S]GTP-gamma-S binding to human KOR expressed in CHO cells	[PMID: 16777411]
CHO	EC₅₀	5.7 1 Compound: U-50488H	Agonist activity at human KOPR expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by liquid scintillation counting Agonist activity at human KOPR expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by liquid scintillation counting	[PMID: 22204910]
CHO	EC₅₀	6.3 1 Compound: U-50488H	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as increase of [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as increase of [35S]GTPgammaS binding	[PMID: 20801035]
CHO	EC₅₀	7.8 1 Compound: U50,488	Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay	[PMID: 30996778]
CHO	EC₅₀	9.31 1 Compound: U-50488	Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay	[PMID: 23134120]
CHO	EC₅₀	13.3 1 Compound: U50,488	Agonist activity at human KOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay Agonist activity at human KOR expressed in CHO cell membranes incubated for 1 hr by [35S]-GTPgammaS coupling assay	[PMID: 31834798]
CHO	EC₅₀	14.4 1 Compound: U-50488	Human Opioid receptor kappa 1 mediated stimulation of [35S]- GTPgammaS binding in CHO cells (Agonist potency). Human Opioid receptor kappa 1 mediated stimulation of [35S]- GTPgammaS binding in CHO cells (Agonist potency).	[PMID: 10893307]
CHO	EC₅₀	21.7 1 Compound: U50488H	Agonist activity at mouse cloned kappa opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay Agonist activity at mouse cloned kappa opioid receptor expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay	[PMID: 24103580]
CHO	ED₅₀	27 1 Compound: (-)-U50,488	Agonist activity against human recombinant opioid kappa receptor expressed in CHO cell membranes after 3 hrs by [35S]GTP-gamma-S binding assay Agonist activity against human recombinant opioid kappa receptor expressed in CHO cell membranes after 3 hrs by [35S]GTP-gamma-S binding assay	[PMID: 25599950]
CHO	EC₅₀	30 1 Compound: (-)-U-50488	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	[PMID: 18380425]
CHO	EC₅₀	36 1 Compound: U-50488	Activity at human cloned kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Activity at human cloned kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 19027293]
CHO	EC₅₀	36 1 Compound: U-50488	Activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding Activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	[PMID: 18417347]
CHO	EC₅₀	36 1 Compound: U50488	Agonist activity at human kappa opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting Agonist activity at human kappa opioid receptor expressed in CHO cell membrane assessed as stimulation of [35S]GTPgammaS binding after 60 mins by liquid scintillation counting	[PMID: 23434225]
CHO	EC₅₀	36 1 Compound: U-50488	Agonist activity at human kappa opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay Agonist activity at human kappa opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay	[PMID: 17935988]
CHO	EC₅₀	36 1 Compound: U-50488	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 60 mins by scintillation counting	[PMID: 23142613]
CHO	EC₅₀	36 1 Compound: U-50488	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	[PMID: 19091564]
CHO	EC₅₀	36 1 Compound: U-50488	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	[PMID: 19282177]
CHO	EC₅₀	36 1 Compound: U-50488	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding	[PMID: 16942039]
CHO	EC₅₀	46 1 Compound: (-)U-50488	Agonist activity at huma kappa opioid receptor expressed in CHO cells assessed as U50488-stimulated of [35S]GTP-gamma-S binding Agonist activity at huma kappa opioid receptor expressed in CHO cells assessed as U50488-stimulated of [35S]GTP-gamma-S binding	[PMID: 17276685]
CHO	EC₅₀	46 1 Compound: U-50488	Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins	[PMID: 17433695]
CHO	EC₅₀	46 1 Compound: U-50488	Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding Agonist activity at human opioid kappa receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding	[PMID: 17407276]
CHO	EC₅₀	80 1 Compound: U50,488	Agonist activity at human KOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay Agonist activity at human KOR expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay	[PMID: 32435376]
HEK293	EC₅₀	1240 1 Compound: U-50488	Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor	[PMID: 17702750]
CHO	EC₅₀	4840 1 Compound: (-)-U-50488	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay	[PMID: 18380425]

分子量

369.33

分子式

C₁₉H₂₆Cl₂N₂O

CAS 番号

67198-13-4

SMILES

ClC(C=C1CC(N([C@H]2[C@H](N3CCCC3)CCCC2)C)=O)=C(C=C1)Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Kumar H, et al. Effect of U50488, a selective kappa opioid receptor agonist and levetiracetam against lithium-pilocarpine-induced status epilepticus, spontaneous convulsive seizures and related cognitive impairment. Neurosci Lett. 2023 Oct 15;815:137477. [Content Brief]

(±)-U-50488 Related Classifications

Neurological Disease

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一般には略語で表示されます：C₁V₁ = C₂V₂

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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.

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(±)-U-5048867198-13-4(±)-trans-(1R,2R)-U-50488Opioid ReceptorInhibitorinhibitorinhibit

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(±)-U-50488 (Synonyms: (±)-trans-(1R,2R)-U-50488)

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(±)-U-50488 (Synonyms: (±)-trans-(1R,2R)-U-50488)

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(±)-U-50488 関連抗体

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•関連小分子:

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Opioid Receptor アイソフォーム固有の製品をすべて表示:

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(±)-U-50488 Related Classifications

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The molarity calculator equation

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