TRPV6
TRPV6 is a highly Ca2+-selective epithelial channel that mediates apical Ca2+ entry during transcellular intestinal calcium absorption[1]. Mechanistically, TRPV6 supports calcium homeostasis under calcium restriction and contributes to bone mineralization in mouse models[2]. In disease research, TRPV6 variants disrupt maternal-fetal calcium transport in transient neonatal hyperparathyroidism and associate with early-onset chronic pancreatitis[3][4]. Compared with TRPV5, TRPV6 shares epithelial Ca2+-channel properties but shows broader tissue distribution, whereas TRPV5 is mainly linked to renal Ca2+ reabsorption[5]. In cancer models, TRPV6 expression correlates with prostate cancer progression, supports prostate cancer cell survival through Orai1-dependent plasma-membrane trafficking, and represents a target in estrogen receptor-negative breast cancer[6][7][8]. For experimental applications, TRPV6 antagonists include SOR-C13/SOR-C27 peptides for detecting TRPV6-rich tumors, SOR-C13 evaluated in a phase I solid-tumor trial, and PCHPD inhibitors that block TRPV6 with nanomolar affinity[9][10][11].
References:
- [1]. Peng JB, et al. Molecular cloning and characterization of a channel-like transporter mediating intestinal calcium absorption. J Biol Chem. 1999 Aug 6;274(32):22739-46. [Content Brief]
- [2]. Lieben L, et al. Trpv6 mediates intestinal calcium absorption during calcium restriction and contributes to bone homeostasis. Bone. 2010 Aug;47(2):301-8. [Content Brief]
- [3]. Suzuki Y, et al. TRPV6 Variants Interfere with Maternal-Fetal Calcium Transport through the Placenta and Cause Transient Neonatal Hyperparathyroidism. Am J Hum Genet. 2018 Jun 7;102(6):1104-1114. [Content Brief]
- [4]. Masamune A, et al. Variants That Affect Function of Calcium Channel TRPV6 Are Associated With Early-Onset Chronic Pancreatitis. Gastroenterology. 2020 May;158(6):1626-1641.e8. [Content Brief]
- [5]. van Abel M, et al. The epithelial calcium channels TRPV5 and TRPV6: regulation and implications for disease. Naunyn Schmiedebergs Arch Pharmacol. 2005 Apr;371(4):295-306. [Content Brief]
- [6]. Fixemer T, et al. Expression of the Ca2+-selective cation channel TRPV6 in human prostate cancer: a novel prognostic marker for tumor progression. Oncogene. 2003 Oct 30;22(49):7858-61. [Content Brief]
- [7]. Raphaël M, et al. TRPV6 calcium channel translocates to the plasma membrane via Orai1-mediated mechanism and controls cancer cell survival. Proc Natl Acad Sci U S A. 2014 Sep 16;111(37):E3870-9. [Content Brief]
- [8]. Peters AA, et al. Calcium channel TRPV6 as a potential therapeutic target in estrogen receptor-negative breast cancer. Mol Cancer Ther. 2012 Oct;11(10):2158-68. [Content Brief]
- [9]. Bowen CV, et al. In vivo detection of human TRPV6-rich tumors with anti-cancer peptides derived from soricidin. PLoS One. 2013;8(3):e58866. [Content Brief]
- [10]. Fu S, et al. First-in-human phase I study of SOR-C13, a TRPV6 calcium channel inhibitor, in patients with advanced solid tumors. Invest New Drugs. 2017 Jun;35(3):324-333. [Content Brief]
- [11]. Bhardwaj R, et al. Inactivation-mimicking block of the epithelial calcium channel TRPV6. Sci Adv. 2020 Nov 27;6(48):eabe1508. [Content Brief]
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TRPV6 Related Products (4)
Related Products (4)
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SOR-C13
0 ImagesSOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity.
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SOR-C13 TFA
0 ImagesCat. No.: HY-P1651APurity: 99.32%SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity.
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TRPV6-IN-1
0 ImagesCat. No.: HY-157574CAS No.: 1819366-84-1TRPV6-IN-1 is a potent and selective TRPV6 inhibitor. TRPV6-IN-1 has anti-proliferative effect and can be used for the research of cancer.
