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SPL-707 

目录号: HY-111360
产品使用指南

SPL-707 是口服有效的,选择性的信号肽肽酶样 2a (SPPL2a) 抑制剂,对 hSPPL2a 的 IC50 为 77 nM。SPL-707 抑制 γ-分泌酶 (γ-secretase; IC50=6.1 μM) 和 SPP (IC50=3.7 μM)。SPL-707 具有靶向 B 细胞和树突状细胞的自身免疫疾病的研究潜力。

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SPL-707 Chemical Structure

SPL-707 Chemical Structure

CAS No. : 2195361-33-0

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Description

SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells[1].

IC50 & Target

IC50: 77 nM (SPPL2a), 6.1 μM (γ-secretase) and 3.7 μM (SPP)[1]

In Vitro

SPL-707 (Compound 40) inhibits mouse SPPL2a (IC50=0.18 μM), rat SPPL2a (IC50=0.056 μM) and human SPPL2a (IC50=0.16 μM), human SPPL2b (IC50=0.43 μM) by a high content imaging assay (HCA)[1].

In Vivo

SPL-707 (Compound 40; 3-30 mg/kg; orally; b.i.d.; for 11 days) leads to a reduction in B cells and myeloid dendritic cells without affecting γ-secretase activity[1].
SPL-707 (3 mg/kg of po and 1 mg/kg of iv) has a CL of 6 mL/min•kg, and an AUC of 8787 h•nM[1].
SPL-707 (1, 3 mg/kg; b.i.d.; first dose at 0 h, second dose at 8 h) achieves full inhibition of CD74/p8 processing in spleen in female Lewis rats[1].

Animal Model: Mice with 5-12 weeks of age[1]
Dosage: 3, 10, and 30 mg/kg
Administration: Orally; b.i.d. (with 8 and 16 h dosing intervals); for 11 days
Result: Led to a reduction in B cells and myeloid dendritic cells without affecting γ-secretase activity.
Animal Model: Female Sprague−Dawley rat[1]
Dosage: 3 mg/kg of po and 1 mg/kg of iv (Pharmacokinetic Analysis)
Administration: PO or IV
Result: Had a CL of 6 mL/min•kg, and an AUC of 8787 h•nM.
Molecular Weight

505.54

Formula

C₂₇H₂₈FN₅O₄

CAS No.

2195361-33-0

SMILES

CC1=C(NC(C[C@@H](C2CC2)C(N[C@@H]3C(N(CC4(CC4)C5)N5C(C6=C3C=CC=C6)=O)=O)=O)=O)C=C(F)C=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

SPL-707SPL707SPL 707Othersorallysignalpeptidepeptidase-like2aSPPL2ahSPPL2aγ-secretaseSPPautoimmuneB cellsdendriticSPPL2bInhibitorinhibitorinhibit

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SPL-707
目录号:
HY-111360
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