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| PHENOLPHTHALEIN DIPHOSPHATE TETRASODIUM Basic information |
| PHENOLPHTHALEIN DIPHOSPHATE TETRASODIUM Chemical Properties |
| Melting point | 98 °C(Solv: methanol (67-56-1); water (7732-18-5)) | | Boiling point | 537.7±50.0 °C(Predicted) | | density | 1.246±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: soluble10mg/mL, clear | | form | powder | | color | white to beige |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36 | | WGK Germany | 3 |
| PHENOLPHTHALEIN DIPHOSPHATE TETRASODIUM Usage And Synthesis |
| Description | Psora 4 is an inhibitor of voltage-gated potassium channels (Kv1.3; EC50 = 3 nM). It is selective for Kv1.3 over Kv1.1, Kv1.2, Kv1.4, Kv1.7, and Kv3.1 channels (EC50s = 62, 49, 202, 100, and 1,500 nM, respectively) but does inhibit the Kv1.5 channel (EC50 = 7.7 nM). Psora 4 selectively binds to the C-type inactivated state of the Kv1.3 channel and inhibits potassium current in a use-dependent manner. It has immunosuppressive activity, inhibiting proliferation of human and rat myelin-specific effector memory T cells in vitro (TEM cells; EC50s = 25 and 60 nM, respectively). | | Uses | Psora-4 is the most potent small-molecule Kv1.3 blocker known. Psora-4 and other Kv1.3 blockers may be useful as immunomodulators for the therapy of autoimmune disorders. | | Biochem/physiol Actions | The lymphocyte potassium channel Kv1.3 is regarded as a new target for immunosuppression. Psora-4 is the most potent small-molecule Kv1.3 blocker known. It blocked Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 value of 3 nM, by preferentially binding to the C-type inactivated state of the channel. It exhibited 17- to 70-fold selectivity for Kv1.3 over closely related Kv1-family channels (Kv1.1, Kv1.2, Kv1.4, and Kv1.7) with the exception of Kv1.5 (EC50, 7.7 nM) and showed no effect on human ether-a-go-go-related channel, Kv3.1, the calcium-activated K+ channels (IKCa1, SK1-SK3, and BKCa), or the neuronal NaV1.2 channel. In a test of in vivo toxicity in rats, Psora-4 did not display any signs of acute toxicity after five daily subcutaneous injections at 33 mg/kg body weight. Psora-4 selectively suppressed the proliferation of human and rat myelin-specific effector memory T cells with EC50 values of 25 and 60 nM, respectively, without persistently suppressing peripheral blood naive and central memory T cells. Because autoantigen-specific effector memory T cells contribute to the pathogenesis of T cell-mediated autoimmune diseases such as multiple sclerosis, Psora-4 and other Kv1.3 blockers may be useful as immunomodulators for the therapy of autoimmune disord. | | in vitro | psora-4 could block kv1.3 in a dose-dependent manner. psora-4 was found to be the most potent small-molecule kv1.3 blocker known. psora-4 exhibited 17- to 70-fold selectivity for kv1.3 over kv1-family channels including kv1.1, kv1.2, kv1.4, and kv1.7 and also showed no effect on human ether-a-go-go-related channel, kv3.1, or the neuronal nav1.2 channel. in addition, psora-4 could suppress the proliferation of rat and human myelin-specific effector memory t cells with ec50 values of 60 and 25 nm, respectively, without persistently suppressing the peripheral blood naive and central memory t cells [1]. | | in vivo | in a study of in vivo toxicity in rats, psora-4 was found not to show any signs of acute toxicity following five daily subcutaneous injections at 33 mg/kg body weight [1]. | | references | [1] vennekamp j,wulff h,beeton c,calabresi pa,grissmer s,hnsel w,chandy kg. kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators. mol pharmacol.2004 jun;65(6):1364-74. |
| PHENOLPHTHALEIN DIPHOSPHATE TETRASODIUM Preparation Products And Raw materials |
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