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TAK-683

Catalog No.: A60972
Metastin/GPR54 Agonist
TAK-683 is a potent full agonist of the KISS1 receptor (KISS1R), exhibiting an IC50 value of 170 pM and a remarkable metabolic stability. As a nonapeptide analog of metastin, TAK-683 demonstrates significant agonistic activity with EC50 values of 0.96 nM and 1.6 nM for human and rat KISS1R, respectively. This compound effectively depletes GnRH in the hypothalamus and subsequently lowers plasma levels of FSH, LH, and testosterone. TAK-683 is valuable for investigating hormone-dependent prostate cancer and related endocrine research applications.
TAK-683 872719-49-8 Metastin/GPR54 Agonist
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Research use only. We do not sell to patients.
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Adooq Products cited in reputable paper
Science VOLUME 380, ISSUE 6663 (2023)
Science VOLUME 369, ISSUE 6510 (2020)
Science VOLUME 356, ISSUE 6336 (2017)
Cell Vol. 185 Issue 23 p4428-4447.e28
Cell Vol 177, Issue 7, p1933-1947.e25
Cell Vol 156, Issue 5, p857-1114
Nature Volume 622 Issue 7982 (2023)
Nature volume 620, pages890-897 (2023)
Nature volume 610, pages540-546 (2022)
Nature volume 588, pages83-88 (2020)
Nature volume 574, pages268-272 (2019)
Nature volume 573, pages539-545 (2019)
Nature volume 567, pages118-122 (2019)
Nature volume 551, pages639-643 (2017)
Nature volume 551, pages247-250 (2017)
Nature volume 548, pages356-360 (2017)
Nature volume 545, pages187-192 (2017)
Biological Activity
DescriptionTAK-683 is a potent full agonist of the KISS1 receptor (KISS1R), exhibiting an IC50 value of 170 pM and a remarkable metabolic stability. As a nonapeptide analog of metastin, TAK-683 demonstrates significant agonistic activity with EC50 values of 0.96 nM and 1.6 nM for human and rat KISS1R, respectively. This compound effectively depletes GnRH in the hypothalamus and subsequently lowers plasma levels of FSH, LH, and testosterone. TAK-683 is valuable for investigating hormone-dependent prostate cancer and related endocrine research applications.
Product Information
Catalog NumA60972
FormulaC64H83N17O13
Molecular Weight1298.45
CAS Number872719-49-8
SequenceN-Acetyl-{d-Tyr}-{d-Trp}-Asn-Thr-Phe-{aza}-Leu-{Met}-Arg-Trp-NH2
Sequence shorteningN-Acetyl--{d-Tyr}-{d-Trp}-NTF-{aza}-L-{Met}-RW-NH2
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
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Endocrinology-Hormones > GPR