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TAK-683

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Catalog No. TP2156LCas No. 872719-49-8

TAK-683 is an effective full KISS1 receptor agonist (IC50=170 pM). TAK-683 is a nonapeptide metastin analog, shows agonistic activities to KISS1R (EC50: 0.96 nM and 1.6 nM for human and rat, respectively).

TAK-683
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TAK-683

😃Good
Catalog No. TP2156LCas No. 872719-49-8
TAK-683 is an effective full KISS1 receptor agonist (IC50=170 pM). TAK-683 is a nonapeptide metastin analog, shows agonistic activities to KISS1R (EC50: 0.96 nM and 1.6 nM for human and rat, respectively).
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Product Introduction

Bioactivity
Description
TAK-683 is an effective full KISS1 receptor agonist (IC50=170 pM). TAK-683 is a nonapeptide metastin analog, shows agonistic activities to KISS1R (EC50: 0.96 nM and 1.6 nM for human and rat, respectively).
Targets&IC50
KISS1R:170 pM
In vitro
In rat KISS1R-expressing Chinese hamster ovary cells, 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 [4].
In vivo
TAK-683 (subcutaneous injection; 0.008, 0.08, 0.8, or 8 μmol/ml/kg; once daily; 7 days) initially increases plasma luteinizing hormone and testosterone levels, but reduces plasma hormones and genital organ weights after 7 days. In a prostate cancer model with TAK-683 (subcutaneous injection; 2.1-21 nmol/kg/day; once daily; 12 weeks), serum PSA concentrations decrease below detection levels (0.5 ng/ml) in all rats by day 14. TAK-683 (subcutaneous injection; 10, 30, or 100 pmol/h; once daily; 4 weeks) shows promise in suppressing reproductive functions and hormone-related diseases such as prostate cancer [3][4].
Chemical Properties
Molecular Weight1298.45
FormulaC64H83N17O13
Cas No.872719-49-8
SmilesC([C@@H](NC([C@@H](CC1=CC=C(O)C=C1)NC(C)=O)=O)C(N[C@H](C(N[C@H](C(N[C@@H](CC2=CC=CC=C2)C(NNC(N[C@H](C(N[C@H](C(N[C@@H](CC=3C=4C(NC3)=CC=CC4)C(N)=O)=O)CCCNC(NC)=N)=O)CC(C)C)=O)=O)=O)[C@@H](C)O)=O)CC(N)=O)=O)C=5C=6C(NC5)=CC=CC6
Relative Density.no data available
SequenceN-Acetyl-{d-Tyr}-{d-Trp}-Asn-Thr-Phe-{aza}-Leu-{Met}-Arg-Trp-NH2
Sequence ShortN-Acetyl--{d-Tyr}-{d-Trp}-NTF-{aza}-L-{Met}-RW-NH2
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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Keywords

TAK-683TAK683TAK 683metastin/GPR54
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