γ6 TM1a trifluoroacetate salt

• Catalog No.: T2955
• CAS Number: 1163243-88-6
• M. F.: C41H73F3N8O11
• M. W.: 911.0605296
• Purity: ≥95% (HPLC)

SYNONYMS

• IUPAC name: (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 Traditional name: (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
• Synonyms: Leu-Gly-Leu-Leu-Val-Ala-Ile-Val trifluoroacetate salt; LGLLVAIV trifluoroacetate salt

DATABASE IDS

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

PROPERTIES

• Empirical Formula (Hill Notation): C39H72N8O9 · xC2HF3O2
• Purity: ≥95% (HPLC)
• Apperance: lyophilized powder
• Solubility: H2O: >1 mg/mL
• Storage Temperature: -20°C
• German water hazard class: 3

DETAILS

Description (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.

Description (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.