Art. -Nr.: HY-130696

(+)-U-50488

(Synonyms: (+)-Trans-(1R,2R)-U-50488)

(+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997).

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CAS. Nr.: 67198-17-8
Formel: C₁₉H₂₆Cl₂N₂O
Molecular Weight:369.33

Speicherung:

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

Data Sheet (268 KB)

(+)-U-50488 Chemical Structure

CAS. Nr.: 67198-17-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

(+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997)^[1].

IC₅₀ & Target^[1]

κ Opioid Receptor/KOR

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

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]

In Vitro

(+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) hydrochloride is a κ opioid receptor agonist that is less active than the (-) trans enantiomer (-)-Trans-(1S,2S)-U-50488 (HY-15997).

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

Chemical Information

CAS. Nr. 67198-17-8
Molecular Weight 369.33
Formel C₁₉H₂₆Cl₂N₂O
SMILES

O=C(N(C)[C@H]1[C@H](N2CCCC2)CCCC1)CC3=CC=C(Cl)C(Cl)=C3
Synonyms

(+)-Trans-(1R,2R)-U-50488
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. DeCosta B, et al. Synthesis and absolute configuration of optically pure enantiomers of a kappa-opioid receptor selective agonist. FEBS Lett. 1987;223(2):335-339. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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(+)-U-50488

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

(+)-U-50488 Related Classifications

HY-130696 Related Classifications