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TAK-683 

Cat. No.: HY-P2161
Handling Instructions

TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.

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TAK-683 Chemical Structure

TAK-683 Chemical Structure

CAS No. : 872719-49-8

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Description

TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively[1]. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer[1][2][4].

IC50 & Target

IC50: 170 pM (metastin/GPR54)[1]

In Vitro

TAK-683 exhibits an IC50 value (95% CI) from receptor binding assays is 150-180 pM and EC50 value (95% CI) from Ca+ mobilization assays is 180 (159–203) pM in rat KISS1R-expressing Chinese hamster ovary (CHO) cells[4].

In Vivo

TAK-683 (subcutaneous injection; 0.008, 0.08, 0.8, or 8 μmol/ml/kg; once daily; 7 days) induces an increase in plasma luteinizing hormone and testosterone levels; however, after day 7, plasma hormone levels and genital organ weights are reduced[3].
TAK-683 (subcutaneous injection; 10, 30, or 100 pmol/h; once daily; 4 weeks) provides a promising for suppressing reproductive functions and hormone-related diseases such as prostate cancer[3].
TAK-683 (subcutaneous injection; 2.1-21 nmol/kg/day; once daily; 12 weeks) has a longer-term evaluation in prostate cancer model, serum concentrations of PSA is reduced in rats, PSA concentrations are reduced to below the limit of detection (0.5 ng/ml)) in all rats by day 14[4].

Animal Model: Male SD rat with prostate cancer model[4]
Dosage: 2.1, 7, 14, 21 nmol/kg/day
Administration: Subcutaneous injection
Result: Exhibited a sustained testosterone suppression in rat.
Molecular Weight

1298.45

Formula

C₆₄H₈₃N₁₇O₁₃

CAS No.

872719-49-8

Sequence

N-Acetyl-{Tyr}{Trp}{Asn}{Thr}{Phe}{aza}{Leu}{Met-Arg}{Trp}-NH2

Sequence Shortening

N-Acetyl-YWNTFGL{Met-R}W-NH2

SMILES

O=C(N)[[email protected]](CC1=CNC2=C1C=CC=C2)NC([[email protected]](CCCNC(NC)=N)NC([[email protected]](CC(C)C)NC(NNC([[email protected]](CC3=CC=CC=C3)NC([[email protected]]([[email protected]](O)C)NC([[email protected]](CC(N)=O)NC([[email protected]@H](CC4=CNC5=C4C=CC=C5)NC([[email protected]@H](CC6=CC=C(O)C=C6)NC(C)=O)=O)=O)=O)=O)=O)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

TAK-683TAK683TAK 683OtherscancerKISSARagonistPSAprostateanalogueGnRHtestosteroneInhibitorinhibitorinhibit

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TAK-683
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