S1P受容体

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S7176 SKI II <1 mg/mL 61 mg/mL '''61 mg/mL
S7177 PF-543 <1 mg/mL 93 mg/mL ''93 mg/mL
S6418 PF 429242 -1 mg/mL 82 mg/mL -1 mg/mL
S7174 Opaganib (ABC294640) <1 mg/mL 76 mg/mL 28 mg/mL
S7791 Phorbol 12-myristate 13-acetate (PMA) <1 mg/mL 100 mg/mL ''100 mg/mL
S6512 Defensamide (MHP) 100 mg/mL 100 mg/mL <1 mg/mL
S5002 Fingolimod (FTY720) HCl 69 mg/mL 69 mg/mL 69 mg/mL
S7182 JTE 013 <1 mg/mL 81 mg/mL 34 mg/mL
S6552 CYM5541 <1 mg/mL 32 mg/mL 63 mg/mL
S7179 Siponimod (BAF312) <1 mg/mL 100 mg/mL ''44 mg/mL
S5950 Fingolimod <1 mg/mL 13 mg/mL 5 mg/mL
S7180 SEW 2871 ' mg/mL
S7952 Ozanimod (RPC1063) <1 mg/mL 81 mg/mL 10 mg/mL
S8241 Ponesimod <1 mg/mL 92 mg/mL 92 mg/mL

亜型選択性的な製品

S1P Receptor製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S7176

SKI II

SKI II is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2.

S7177

PF-543

PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 induces apoptosis, necrosis, and autophagy.

S6418

PF 429242

PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).

S7174

Opaganib (ABC294640)

Opaganib (ABC294640) is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM. Phase 1/2.

S7791

Phorbol 12-myristate 13-acetate (PMA)

Phorbol 12-myristate 13-acetate (PMA), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).

S6512

Defensamide (MHP)

Defensamide (MHP) is an activator of sphingosine kinase (SPHK1). It can modulate the innate epidermal immune response by potentiating SPHK1 activity and inducing cAMP production.

S5002

Fingolimod (FTY720) HCl

Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.

S7182

JTE 013

JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.

S6552

CYM5541

CYM5541 is a selective, allosteric agonist of S1P3 with an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes in vitro: S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM.

S7179

Siponimod (BAF312)

BAF312 (Siponimod) is a next-generation S1P receptor modulator, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.

S5950

Fingolimod

Fingolimod is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.

S7180

SEW 2871

Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.

S7952

Ozanimod (RPC1063)

Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3.

S8241

Ponesimod

Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S7176

SKI II

SKI II is a highly selective and non ATP-competitive sphingosine kinase (SphK) inhibitor with IC50 of 0.5 μM, while exhibiting no inhibitory action on other kinases including PI3K, PKCα and ERK2.

S7177

PF-543

PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM, exhibits >100-fold selectivity over the SphK2 isoform. PF-543 induces apoptosis, necrosis, and autophagy.

S6418

PF 429242

PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).

S7174

Opaganib (ABC294640)

Opaganib (ABC294640) is an orally bioavailable and selective sphingosine kinase-2 (SphK2) inhibitor with IC50 of approximately 60 μM. Phase 1/2.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S7791

Phorbol 12-myristate 13-acetate (PMA)

Phorbol 12-myristate 13-acetate (PMA), a potent activator of PKC, is active at nanomolar concentrations. Phorbol 12-myristate 13-acetate (PMA) induces sphingosine-1-phosphate (S1P).

2020, 4

2020, 11:754

2020, 40(4)

S6512

Defensamide (MHP)

Defensamide (MHP) is an activator of sphingosine kinase (SPHK1). It can modulate the innate epidermal immune response by potentiating SPHK1 activity and inducing cAMP production.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S5002

Fingolimod (FTY720) HCl

Fingolimod (FTY720) HCl is a S1P antagonist with IC50 of 0.033 nM in K562, and NK cells.

2020, 24

2020, 468:1-13

2020, 8;11:635

S7182

JTE 013

JTE 013 is a potent and selective S1P2 antagonist with IC50 of 17.6 nM.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S6552

CYM5541

CYM5541 is a selective, allosteric agonist of S1P3 with an EC50 of between 72 and 132 nM and exhibits exquisite selectivity over other S1P receptor subtypes in vitro: S1P1 EC50 > 10 μM, S1P2 EC50 > 50 μM, S1P4 EC50 > 50 μM, and S1P5 EC50 > 25 μM.

S7179

Siponimod (BAF312)

BAF312 (Siponimod) is a next-generation S1P receptor modulator, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.

2020, 8;11:635

2020, 15:5561-5571

2019, 10.1038/s41375-019-0478-9

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S5950

Fingolimod

Fingolimod is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.

2020, 8;11:635

2020, 4(12):2595-2605

2020, 10.1038/s41385-020-0327-1

S7180

SEW 2871

Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.

S7952

Ozanimod (RPC1063)

Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3.

2019, 10.1093/nar/gkz1136

2019, 10.1038/s41375-019-0478-9

2019, 10.1038/s41375-019-0511-z

S8241

Ponesimod

Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.

2020, 10.1002/2211-5463.12951

2019, 10.1038/s41375-019-0478-9