γ6 TM1a trifluoroacetate salt

• 产品号: T2955
• CAS号: 1163243-88-6
• 分子式: C41H73F3N8O11
• 分子量: 911.0605296
• 纯 度: ≥95% (HPLC)

产品别名

• 标题: γ6 TM1a trifluoroacetate salt
• IUPAC标准名: (2S)-2-{2-[(1S,2S)-1-{[(1R)-1-{[(1S)-1-{[(4S,7S)-7-{2-[(2S)-2-amino-4-methylpentanamido]acetamido}-2,9-dimethyl-5,6-dioxodecan-4-yl]carbamoyl}-2-methylpropyl]carbamoyl}ethyl]carbamoyl}-2-methylbutyl]hydrazin-1-yl}-3-methylbutanoic acid; trifluoroacetic acid
• IUPAC传统名: (2S)-2-{2-[(1S,2S)-1-{[(1R)-1-{[(1S)-1-{[(4S,7S)-7-{2-[(2S)-2-amino-4-methylpentanamido]acetamido}-2,9-dimethyl-5,6-dioxodecan-4-yl]carbamoyl}-2-methylpropyl]carbamoyl}ethyl]carbamoyl}-2-methylbutyl]hydrazin-1-yl}-3-methylbutanoic acid; trifluoroacetic acid
• 别名: Leu-Gly-Leu-Leu-Val-Ala-Ile-Val trifluoroacetate salt; LGLLVAIV trifluoroacetate salt

产品登记号

• MDL号: MFCD17215947
• CAS号: 1163243-88-6

产品性质

• Empirical Formula (Hill Notation): C39H72N8O9 · xC2HF3O2
• 纯度: ≥95% (HPLC)
• 外观: lyophilized powder
• 溶解度: H2O: >1 mg/mL
• 保存温度: -20°C
• 德国WGK号: 3

产品详细信息

详细说明 (简体中文)

Amino Acid Sequence
Leu-Gly-Leu-Leu-Val-Ala-Ile-Val
Biochem/physiol Actions
The calcium channel γ family is a subgroup of the tetraspanin proteins. There are the eight γ subunits that have been identified to date. Among these γ1 subunit acts as an endogenous antagonist of the skeletal HVA calcium current, and γ6 inhibits the low voltage-activated (LVA) Cav3.1 calcium current. A GxxxA motif in the first transmembrane domain (TM1) of γ6 was identified as critical for inhibiting the Cav3.1 current. γ6 TM1a is an octapeptide contains residues 41 through 48 of the native γ6 protein. The peptide inhibits the Cav3.1 calcium current in a dose-dependent manner. The reduction of channel current is mostly due to the inhibition of both resting and inactivated channels relatively independent of membrane potential. Thus γ6 TM1might function as a pore blocker. Also γ6 TM1a peptide inhibits Cav1.2 current with reduced efficacy. The γ6 TM1a peptide has the potential of being further developed as a novel therapeutic agent targeting Cav3.1 and possibly Cav1.2 calcium current.

详细说明 (English)

Amino Acid Sequence
Leu-Gly-Leu-Leu-Val-Ala-Ile-Val
Biochem/physiol Actions
The calcium channel γ family is a subgroup of the tetraspanin proteins. There are the eight γ subunits that have been identified to date. Among these γ1 subunit acts as an endogenous antagonist of the skeletal HVA calcium current, and γ6 inhibits the low voltage-activated (LVA) Cav3.1 calcium current. A GxxxA motif in the first transmembrane domain (TM1) of γ6 was identified as critical for inhibiting the Cav3.1 current. γ6 TM1a is an octapeptide contains residues 41 through 48 of the native γ6 protein. The peptide inhibits the Cav3.1 calcium current in a dose-dependent manner. The reduction of channel current is mostly due to the inhibition of both resting and inactivated channels relatively independent of membrane potential. Thus γ6 TM1might function as a pore blocker. Also γ6 TM1a peptide inhibits Cav1.2 current with reduced efficacy. The γ6 TM1a peptide has the potential of being further developed as a novel therapeutic agent targeting Cav3.1 and possibly Cav1.2 calcium current.