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  2. TAK-683 TFA

TAK-683 TFA 

Cat. No.: HY-P2161A
Handling Instructions

TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA 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 TFA 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.

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

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TAK-683 TFA Chemical Structure

TAK-683 TFA Chemical Structure

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Description

TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA 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 TFA 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][3].

IC50 & Target

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

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[1].
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[1].
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[1].

Animal Model: Male SD rat with prostate cancer model[1]
Dosage: 2.1, 7, 14, 21 nmol/kg/day
Administration: Subcutaneous injection
Result: Exhibited a sustained testosterone suppression in rat.
Molecular Weight

1412.47

Formula

C₆₆H₈₄F₃N₁₇O₁₅

Sequence

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

Sequence Shortening

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

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 TFA
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HY-P2161A
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