TAK-683

Name: TAK-683
Brand: TargetMol
SKU: TP2156L
Rating: 4.5 (1 reviews)

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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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Catalog No. TP2156LCas No. 872719-49-8

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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 Weight	1298.45
Formula	C₆₄H₈₃N₁₇O₁₃
Cas No.	872719-49-8
Smiles	C([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
Sequence	N-Acetyl-{d-Tyr}-{d-Trp}-Asn-Thr-Phe-{aza}-Leu-{Met}-Arg-Trp-NH2
Sequence Short	N-Acetyl--{d-Tyr}-{d-Trp}-NTF-{aza}-L-{Met}-RW

Storage & Solubility Information

Storage

keep 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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc