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Cat. No.: HY-117982

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SKI2496

SKI2496 is an orally active GnRH receptor antagonist (IC₅₀: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca²⁺ flux with an IC₅₀ value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC₅₀ value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders.

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CAS No.: 1308378-95-1
Formule: C₃₅H₃₆F₇N₅O₅
Masse moléculaire:739.68

Stockage:

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

Data Sheet (268 KB)

SKI2496 Chemical Structure

CAS No.: 1308378-95-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform ERK :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	0.44 nM Compound: 18a	Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay	[PMID: 27608177]
HEK293	IC₅₀	13 nM Compound: 18a	Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs b Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs b	[PMID: 27608177]
HEK293	IC₅₀	13.2 nM Compound: 18a	Antagonist activity against monkey GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 10 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs Antagonist activity against monkey GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 10 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs	[PMID: 27608177]
HEK293	IC₅₀	2.9 nM Compound: 18a	Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay	[PMID: 27608177]
HEK293	IC₅₀	279.2 nM Compound: 18a	Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by l Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by l	[PMID: 27608177]
HEK293	IC₅₀	3.7 nM Compound: 18a	Displacement of [125I]D-Trp6-LHRH from monkey GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay Displacement of [125I]D-Trp6-LHRH from monkey GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay	[PMID: 27608177]
HEK293	IC₅₀	520 nM Compound: 18a	Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay	[PMID: 27608177]
HEK293	IC₅₀	6.32 nM Compound: 18a	Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by	[PMID: 27608177]

Chemical Information

CAS No. 1308378-95-1
Masse moléculaire 739.68
Formule C₃₅H₃₆F₇N₅O₅
SMILES

O=C(O)CCCN[C@H](C1=CC=CC=C1)CN(C(N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C3N4CCN(CC5=CC=C(C(F)(F)F)O5)CC4)=O)C3=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[1]. Kim SM, et al. Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. J Med Chem. 2016 Oct 13;59(19):9150-9172. [Content Brief]

Calculators

Calculateur de molarité

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

Mass Mass

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Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Concentration _(final) Concentration _(final)

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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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100 mg

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Activité biologique
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Chemical Information
Pureté et documentation
Références

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SKI2496

Voir tous les produits spécifiques à Isoform ERK

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

SKI2496 Related Classifications

HY-117982 Related Classifications