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

Cat. No.: HY-130696A: Data Sheet Handling Instructions
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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.

For research use only. We do not sell to patients.

(±)-U-50488 Chemical Structure

CAS No. : 67198-13-4

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Other Forms of (±)-U-50488:

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

κ Opioid Receptor/KOR

Cellular Effect

Cell Line	Type	Value	Description	References
C6	IC₅₀	1.99 nM 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	EC₅₀	1.4 nM 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 nM 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]
CHO	EC₅₀	13.3 nM 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 nM 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	2.9 nM 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	21.7 nM 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	EC₅₀	3.4 nM 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	3.4 nM 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	30 nM 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 nM 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 nM 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	36 nM 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 nM 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 nM 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 nM 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 nM 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 nM 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	4.2 nM 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 nM 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	46 nM 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 nM 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	46 nM 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	4840 nM 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]
CHO	EC₅₀	5.7 nM 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 nM 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 nM 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	80 nM 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]
CHO	EC₅₀	9.31 nM 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	ED₅₀	27 nM 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	IC₅₀	6.4 × 10^-10M 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	IC₅₀	6.4 × 10^-10M 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]
HEK293	EC₅₀	1240 nM 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]
HEK293	IC₅₀	0.3 nM 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]
HEK293	IC₅₀	0.9 nM 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]
HEK-293T	IC₅₀	0.3 nM 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]

Molecular Weight

369.33

Formula

C₁₉H₂₆Cl₂N₂O

CAS No.

67198-13-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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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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:

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

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