GPBAR1


Proteins
Membrane proteins are the most pharmaceutically relevant protein class. At the same time, it is very difficult to obtain them in pure, active form. Cube Biotech's protein experts have worked hard to produce human GPCRs in sufficient quality that we can now offer to the community. Our first available pure, active membrane protein is GPBAR1 / TGR5, a human GPCR involved in bile acid homeostasis, glucose metabolism, and weight maintenance. The protein is available off-the shelf, ready for ligand binding studies, crystallization, and other biochemical/biophysical experiments.

TGR5_SDS-Page
Fig. 1: SDS-PAGE of GPBAR1, purified via Rho1D4 affinity chromatography. L: Lysate: FT: flow through, W: Wash, E1-E3: elution fractions with purified GPCR.
TGR5_absorbance_spectrum
Fig. 2: Surface plasmon resonance measurement of GPBAR-1 / Taurolithocholic acid sulfate salt interaction. Using a 1:1 binding model, the Kd was determined to be 1.1x10e-8 M.

 

Features

Protein GPBAR1 (G-protein coupled bile receptor 1)
Alternative names TGR5, GPCR19, M-BAR, BG37
UniProt / UniGene Q8TDU6 / 155918
Protein class GPCR, class A (Rhodopsin-like receptors)
Organism Human (Homo sapiens)
Sequence

Full-length, wildtype sequence N-terminal HA tag (underlined), 10x His-tag with spacer (red), HRV 3C protease site (blue) spacer (gray), Rho1D4 tag (green)


MKTIIALSYIFCLVFAMTPNSTGEVPSPIPKGALGLSLALASLIIT ANLLLALGIA WDRRLRSPPA GCFFLSLLLA GLLTGLALPT LPGLWNQSRR GYWSCLLVYL APNFSFLSLL ANLLLVHGER YMAVLRPLQP PGSIRLALLL TWAGPLLFAS LPALGWNHWT PGANCSSQAI FPAPYLYLEV YGLLLPAVGA AAFLSVRVLA TAHRQLQDIC RLERAVCRDE PSALARALTW RQARAQAGAM LLFGLCWGPY VATLLLSVLA YEQRPPLGPG TLLSLLSLGS ASAAAVPVAM GLGDQRYTAP WRAAAQRCLQ GLWGRASRDS PGPSIAYHPS SQSSVDLDLNGGHHHHHHHHHHLEVLFQGPGS SGTETSQVAPA

Affinity tags His / Rho1D4 (both C-terminal)
Size (excluding additional elements) 379 (330) amino acids 40,606 (35,248) Da
Expression system Sf9 (baculovirus)
Purified via PureCube Rho1D4 Agarose
Buffer 100 mM NaCl, 20 mM NaH2PO4 pH 7.4, 0.1% Foscholine-12, 0.01% cholesterolhemisuccinate (CHS)
Purity (SDS-PAGE) >98%, see Fig. 1
Homogeneity Size exclusion chromatography
Activity Ligand binding measured by SPR using Taurolithocholic Acid Sulfate Disodium Salt (CAS 64936-83-0) at 10°C. Using a 1:1 binding model, the dissociation constant (Kd) was determined to be 1.1x10e-8 M.
Function Receptor for bile acid. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production. May be involved in the suppression of macrophage functions by bile acids, and in modulating inflammation.
Literature references
  1. Kawamata, Yuji, et al. "AG protein-coupled receptor responsive to bile acids." Journal of Biological Chemistry 278.11 (2003): 9435-9440.
Proteins
Membrane proteins are the most pharmaceutically relevant protein class. At the same time, it is very difficult to obtain them in pure, active form. Cube Biotech's protein experts have worked hard to produce human GPCRs in sufficient quality that we can now offer to the community. Our first available pure, active membrane protein is GPBAR1 / TGR5, a human GPCR involved in bile acid homeostasis, glucose metabolism, and weight maintenance. The protein is available off-the shelf, ready for ligand binding studies, crystallization, and other biochemical/biophysical experiments.

TGR5_SDS-Page
Fig. 1: SDS-PAGE of GPBAR1, purified via Rho1D4 affinity chromatography. L: Lysate: FT: flow through, W: Wash, E1-E3: elution fractions with purified GPCR.
TGR5_absorbance_spectrum
Fig. 2: Surface plasmon resonance measurement of GPBAR-1 / Taurolithocholic acid sulfate salt interaction. Using a 1:1 binding model, the Kd was determined to be 1.1x10e-8 M.

 

Features

Protein GPBAR1 (G-protein coupled bile receptor 1)
Alternative names TGR5, GPCR19, M-BAR, BG37
UniProt / UniGene Q8TDU6 / 155918
Protein class GPCR, class A (Rhodopsin-like receptors)
Organism Human (Homo sapiens)
Sequence

Full-length, wildtype sequence N-terminal HA tag (underlined), 10x His-tag with spacer (red), HRV 3C protease site (blue) spacer (gray), Rho1D4 tag (green)


MKTIIALSYIFCLVFAMTPNSTGEVPSPIPKGALGLSLALASLIIT ANLLLALGIA WDRRLRSPPA GCFFLSLLLA GLLTGLALPT LPGLWNQSRR GYWSCLLVYL APNFSFLSLL ANLLLVHGER YMAVLRPLQP PGSIRLALLL TWAGPLLFAS LPALGWNHWT PGANCSSQAI FPAPYLYLEV YGLLLPAVGA AAFLSVRVLA TAHRQLQDIC RLERAVCRDE PSALARALTW RQARAQAGAM LLFGLCWGPY VATLLLSVLA YEQRPPLGPG TLLSLLSLGS ASAAAVPVAM GLGDQRYTAP WRAAAQRCLQ GLWGRASRDS PGPSIAYHPS SQSSVDLDLNGGHHHHHHHHHHLEVLFQGPGS SGTETSQVAPA

Affinity tags His / Rho1D4 (both C-terminal)
Size (excluding additional elements) 379 (330) amino acids 40,606 (35,248) Da
Expression system Sf9 (baculovirus)
Purified via PureCube Rho1D4 Agarose
Buffer 100 mM NaCl, 20 mM NaH2PO4 pH 7.4, 0.1% Foscholine-12, 0.01% cholesterolhemisuccinate (CHS)
Purity (SDS-PAGE) >98%, see Fig. 1
Homogeneity Size exclusion chromatography
Activity Ligand binding measured by SPR using Taurolithocholic Acid Sulfate Disodium Salt (CAS 64936-83-0) at 10°C. Using a 1:1 binding model, the dissociation constant (Kd) was determined to be 1.1x10e-8 M.
Function Receptor for bile acid. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production. May be involved in the suppression of macrophage functions by bile acids, and in modulating inflammation.
Literature references
  1. Kawamata, Yuji, et al. "AG protein-coupled receptor responsive to bile acids." Journal of Biological Chemistry 278.11 (2003): 9435-9440.
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GPBAR1 (TGR5) protein GPBAR1 (TGR5) protein
Article number: 28101
GPBAR1
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GPBAR1 (TGR5) protein GPBAR1 (TGR5) protein
Active, purified membrane protein GPBAR1 (TGR1) from human. 10 or 50 µg in solution. Ready to ship and use for your research.
Article number: 28101
Sales price: From €1,018.00 *
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