Nucleotide Analogs - Jena Bioscience

The human leukotriene B4 receptor (BLTR) is a seven
transmembrane-domain (7TM), G protein-coupled
receptor (GPCR). Leukotriene B4 (LTB4) is a potent
chemoattractant active on multiple leukocytes,
including neutrophils, macrophages, and eosinophils.
LTB4 is involved in the pathogenesis of a wide variety
of human infl ammatory diseases. Therefore, the
BLTR represents an attractive target for therapeutic
intervention.
BLTR reconstituted with the G-protein G i á 2 α 1 ã 2 was
prepared from Sf9 cells triple-infected with BLTR-,
G iá 2-, and Gα 1ã 2-encoding baculoviruses.
The BLTR contains a N-terminal FLAG-Tag ®
and a C-terminal hexahistidine (His6)-Tag for
immunochemical detection and protection against
proteolysis.
Protein concentration: 0.8 – 1.3 mg/ml
Store: -80 °C
Selected references:
Yokomizo et al. (1997) A G-protein-coupled receptor for
leukotriene B4 that mediates chemotaxis. Nature 387:620.
Tager et al. (2000) BLTR mediates leukotriene B4-induced
chemotaxis and adhesion and plays a dominant role in
eosinophil accumulation in a murine model of peritonitis. J.
Exp. Med. 192:439.
Seifert, R. and Wenzel-Seifert, K. (2001) Unmasking different
constitutive activity of four chemoattractant receptors using
Na + as universal stabilizer of the inactive (R) state. Receptors
Channels 7:357.
Leukotriene B4 receptor
(BLTR) + co-expressed
G-protein G i α 3 β 1 γ 2 complex
human, Recombinant, Sf9
insect cells
Cat. No. Amount Price (€)
PR-562 1 ml 300,--
Membrane suspension. Supplied in 75 mM Tris-HCl,
pH 7.4, 12.5 mM MgCl 2 , and 1 mM EDTA.
The human leukotriene B4 receptor (BLTR) is a seven
transmembrane-domain (7TM), G protein-coupled
receptor (GPCR). Leukotriene B4 (LTB4) is a potent
chemoattractant active on multiple leukocytes,
including neutrophils, macrophages, and eosinophils.
LTB4 is involved in the pathogenesis of a wide variety
of human infl ammatory diseases. Therefore, the
BLTR represents an attractive target for therapeutic
intervention.
BLTR reconstituted with the G-protein G iα 3β 1γ 2 was
prepared from Sf9 cells triple-infected with BLTR-,
G iα 3-, and Gβ 1γ 2-encoding baculoviruses.
The BLTR contains a N-terminal FLAG-Tag ®
and a C-terminal hexahistidine (His6)-Tag for
immunochemical detection and protection against
proteolysis.
Protein concentration: 1.5 mg/ml
Store: -80 °C
Selected references:
Yokomizo et al. (1997) A G-protein-coupled receptor for
leukotriene B4 that mediates chemotaxis. Nature 387:620.
Tager et al. (2000) BLTR mediates leukotriene B4-induced
chemotaxis and adhesion and plays a dominant role in
eosinophil accumulation in a murine model of peritonitis. J.
Exp. Med. 192:439.
Seifert, R. and Wenzel-Seifert, K. (2001) Unmasking different
constitutive activity of four chemoattractant receptors using
Na + as universal stabilizer of the inactive (R) state. Receptors
Channels 7:357.
Histamine Receptors
Histamine H 1 -Receptor (H 1 R)
guinea pig, Recombinant, Sf9
insect cells
Cat. No. Amount Price (€)
PR-611 1 ml 300,--
Membrane suspension. Supplied in 75 mM Tris-HCl,
pH 7.4, 12.5 mM MgCl 2 , and 1 mM EDTA.
The histamine H 1-receptor (H 1R) belongs to the
superfamily of seven transmembrane-domain
(7TM), G-protein-coupled receptors (GPCRs). The
endogenous agonist for the H 1 R is histamine which is
both neurotransmitter and autacoid. The H 1R couples
to G q-proteins to activate phospholipase C.
Numerous agonists and antagonists are known. H 1 R
agonists are divided into three classes, i.e. small
agonists derived from histamine, histamine derivatives
with bulkier aromatic substituents at position 2 of the
imidazole ring and histaprofi dens. H 1R antagonists are
commonly divided into sedating (fi rst-generation) and
nonsedating (second-generation) antagonists. Today,
especially the second-generation H 1 R antagonists
are of great importance for the treatment of allergic
diseases. Guanidines derived from arpromidine
are dual H 2 R agonists/H 1 R antagonists. Small H 1 R
agonists exhibit similar effects at human H 1 R (hH 1 R,
cat.# PR-614) and guinea pig H 1 R (gpH 1 R), whereas
bulkier 2-phenylhistamines and histaprodifens are
up to ~10-fold more potent at gpH 1 R than at hH 1 R.
Several fi rst-generation H 1 R antagonists are ~2-fold,
and arpromidine-type H 1 R antagonists up to ~10-fold
more potent at gpH 1 R than at hH 1 R. gpH 1 R was
prepared from Sf9 cells infected with gpH 1 R-encoding
baculovirus.
gpH 1 R contains a N-terminal FLAG-Tag ® and a
C-terminal hexahistidine (His6)-Tag for immunological
detection, to allow purifi cation, and to provide
additional protection against proteolysis.
Protein concentration: 1 – 1.4 mg/ml
Store: -80 °C
Selected references:
Houston et al. (2002) The human histamine H 2 -receptor
couples more effi ciently to Sf9 insect cell G s -proteins than to
insect cell G q -proteins: limitations of Sf9 cells for the analysis of
receptor/G q -protein coupling. J. Neurochem. 80:678.
Seifert et al. (2003) Multiple differences in agonist and
antagonist pharmacology between human and guinea pig
histamine H 1 -receptor. J. Pharmacol. Exp. Ther. 305:1104.
Leopoldt et al. (1997) G Proteins endogenously expressed
in Sf9 cells: interaction with mammalian histamine receptors.
Naunyn- Schmiedeberg’s Arch. Pharmacol. 356:216.
Horio et al. (1993) Molecular cloning of the guinea-pig histamine
H 1 receptor gene. J. Biochem. (Tokyo) 114:408.
Histamine H 1 -Receptor
(H 1 R) + co-expressed RGS4
guinea pig, Recombinant, Sf9
insect cells
Cat. No. Amount Price (€)
PR-612 1 ml 300,--
Membrane suspension. Supplied in 75 mM Tris-HCl,
pH 7.4, 12.5 mM MgCl 2 , and 1 mM EDTA.
The histamine H 1 -receptor (H 1 R) belongs to the
superfamily of seven transmembrane-domain
(7TM), G-protein-coupled receptors (GPCRs). The
endogenous agonist for the H 1 R is histamine which is
both neurotransmitter and autacoid. The H 1 R couples
to G q -proteins to activate phospholipase C.
Numerous agonists and antagonists are known. H 1 R
agonists are divided into three classes, i.e. small
agonists derived from histamine, histamine derivatives
with bulkier aromatic substituents at position 2 of the
GTP Signal Transduction
imidazole ring and histaprofi dens. H 1 R antagonists are
commonly divided into sedating (fi rst-generation) and
nonsedating (second-generation) antagonists. Today,
especially the second-generation H 1 R antagonists
are of great importance for the treatment of allergic
diseases. Guanidines derived from arpromidine
are dual H 2 R agonists/H 1 R antagonists. Small H 1 R
agonists exhibit similar effects at human H 1 R (hH 1 R)
and guinea pig H 1 R (gpH 1 R), whereas bulkier
2-phenylhistamines and histaprodifens are up to
~10-fold more potent at gpH 1 R than at hH 1 R. Several
fi rstgeneration H 1R antagonists are ~2-fold, and
arpromidine-type H 1 R antagonists up to ~10-fold more
potent at gpH 1 R than at hH 1 R.
The regulator of G-protein signalling 4 (RGS4)
effi ciently enhances steady-state GTP hydrolysis
stimulated by H 1 R, thus providing a very sensitive
model system for the pharmacological analysis of the
H 1 R directly at the G-protein level.
gpH 1 R + RGS4 were prepared from Sf9 cells coinfected
with gpH 1 R- and RGS4-encoding baculoviruses.
The protein contains a N-terminal FLAG-Tag ® and a
C-terminal hexahistidine (His6)-Tag for immunological
detection and protection against proteolysis.
Protein concentration: 2.2 mg/ml
Store: -80 °C
Selected references:
Houston et al. (2002) The human histamine H 2 -receptor
couples more effi ciently to Sf9 insect cell G s -proteins than to
insect cell G q -proteins: limitations of Sf9 cells for the analysis of
receptor/G q -protein coupling. J. Neurochem. 80:678.
Seifert et al. (2003) Multiple differences in agonist and
antagonist pharmacology between human and guinea pig
histamine H 1 -receptor. J. Pharmacol. Exp. Ther. 305:1104.
Leopoldt et al. (1997) G Proteins endogenously expressed
in Sf9 cells: interaction with mammalian histamine receptors.
Naunyn- Schmiedeberg’s Arch. Pharmacol. 356:216.
Horio et al. (1993) Molecular cloning of the guinea-pig histamine
H 1 receptor gene. J. Biochem. (Tokyo) 114:408.
Ross EM and Wilkie TM (2000) GTPase-activating proteins
for heterotrimeric G proteins: regulators of G protein signaling
(RGS) and RGS-like proteins. Annu. Rev. Biochem. 69:795.
Histamine H 2-Receptor (H 2R)
guinea pig, Recombinant, Sf9
insect cells
Cat. No. Amount Price (€)
PR-613 1 ml 300,--
Membrane suspension. Supplied in 75 mM Tris-HCl,
pH 7.4, 12.5 mM MgCl 2, and 1 mM EDTA.
The histamine H 2-receptor (H 2R) belongs to the
superfamily of seven transmembrane domain
(7TM), G-protein-coupled receptors (GPCRs). The
endogenous agonist for the H 2R is histamine which is
both neurotransmitter and autacoid. The H 2 R couples
to G s -proteins to mediate adenylate cyclase (AC)
activation. In some systems, the H 2 R also couples
to G q -proteins and phospholipase C. Among the
many responses mediated by the H 2 R are gastric
acid secretion, smooth muscle relaxation, positive
ionotropic and chronotropic effects on heart muscle,
and inhibition of leukocyte function.
The guinea pig H 2 R (gpH 2 R) was prepared from Sf9
cells infected with gpH 2 R-encoding baculovirus. In this
system, gpH 2 R couples to the G sα -like G-proteins of
the insect cells to mediate AC activation.
gpH 2 R contains a N-terminal FLAG-Tag ® and a
C-terminal hexahistidine (His6)-Tag for immunological
detection, to allow purifi cation, and to provide
additional protection against proteolysis.
Protein concentration: 0.8 mg/ml
Store: -80 °C
Selected references:
Houston et al. (2002) The human histamine H 2 -receptor
couples more effi ciently to Sf9 insect cell G s -proteins than to
insect cell G q -proteins: limitations of Sf9 cells for the analysis of
receptor/G q -protein coupling. J. Neurochem. 80:678.
Leopoldt et al. (1997) G Proteins endogenously expressed
in Sf9 cells: interaction with mammalian histamine receptors.
Recombinant Proteins
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