盐酸脒基吡唑(扎那米韦杂质)
英文名称 | 1H-Pyrazole-1-carboxamidine Hydrochloride |
CAS | 4023-02-3 |
储存条件 | RT |
单位 | 瓶 |
规格 | 50mg |
盐酸脒基吡唑(扎那米韦杂质)
英文名称 | 1H-Pyrazole-1-carboxamidine Hydrochloride |
CAS | 4023-02-3 |
储存条件 | RT |
单位 | 瓶 |
规格 | 50mg |
吡唑(扎那米韦杂质)
英文名称 | Pyrazole |
CAS | 288-13-1 |
储存条件 | 2-8℃ |
单位 | 瓶 |
规格 | 50mg |
西地那非 标准品
英文名称 | Sildenafil |
CAS | 139755-83-2 |
分子式 | C22H30N6O4S |
分子量 | 474.58 |
储存条件 | 2-8℃ |
规格 | 100mg |
熔点:187-189°C
1-叔丁基-3-(1-萘基)-1H-吡唑并[3,4-d]嘧啶-4-胺盐酸盐,1-Naphthyl PP1 (hydrochloride),CAS:956025-47-1,货号:IN0290-5mg
市场价: | ¥1120.0 | |
价格: |
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品牌: | solarbio | |
规格: | 5mg |
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说明书下载
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1-叔丁基-3-(1-萘基)-1H-吡唑并[3,4-d]嘧啶-4-胺盐酸盐,,CAS:956025-47-1,货号:IN0290-10mM*1mL (in DMSO)
市场价: | ¥1320.0 | |
价格: |
|
|
品牌: | solarbio | |
规格: | 10mM*1mL (in DMSO) |
产品详情
说明书下载
参考文献
|
1-叔丁基-3-(1-萘基)-1H-吡唑并[3,4-d]嘧啶-4-胺盐酸盐,1-Naphthyl PP1 (hydrochloride),CAS:956025-47-1,货号:IN0290-10mg
市场价: | ¥2000.0 | |
价格: |
|
|
品牌: | solarbio | |
规格: | 10mg |
产品详情
说明书下载
参考文献
|
磺胺苯吡唑
有效期 | 2年 |
MDL | MFCD00057226 |
EC | EINECS 208-384-3 |
InChIKey | QWCJHSGMANYXCW-UHFFFAOYSA-N |
InChI | InChI=1S/C15H14N4O2S/c16-12-6-8-14(9-7-12)22(20,21)18-15-10-11-17-19(15)13-4-2-1-3-5-13/h1-11,18H,16H2 |
PubChem CID | 5335 |
别名 | 苯磺酰胺 |
英文名称 | Sulfaphenazole |
CAS | 526-08-9 |
分子式 | C15H14N4O2S |
分子量 | 314.36 |
储存条件 | 2-8℃ |
纯度 | ≥98% |
外观(性状) | White to pale yellow Powder |
单位 | 瓶 |
生物活性 | Sulfaphenazole (Depocid, Depotsulfonamide, Plisulfan, Raziosulfa) is an inhibitor of CYP2C9 with Ki value of 0.3 μM and demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki values of 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).[1-2] |
In Vitro | Cystamine is a transglutaminase (TGase) inhibitor. In addition to TGase inhibition, cystamine is able to replenish glutathione and to inhibit caspase activity. The inhibitory capacity of cystamine in vitro is largely affected by the extent of the reduced form of the molecule. Nonetheless, cystamine inhibits in situ TGase activity decidedly stronger than cysteamine[1]. |
In Vivo | Treatment with cystamine results in prolonged survival and decreased abnormal movements in a murine model of HD(Huntington’s disease). Cystamine does not cross the blood brain barrier[1]. Cystamine treatment normalizes transglutaminase and GGEL levels in R6/2 mice. cystamine has significant efficacy in improving the neurological and neuropathological phenotype observed in the R6/2 transgenic model of HD and strongly suggests that Tgase plays a role in HD[2]. |
SMILES | O=S(C1=CC=C(N)C=C1)(NC2=CC=NN2C3=CC=CC=C3)=O |
靶点 | CYP2C9 |
动物实验 | The cells (2×106) are labeled with BP at 1 mM or amine compounds (0 to 1.0 mM) in serum-free medium for 1h prior to harvesting. After washing twice with PBS, the cells are suspended in PBS containing protease inhibitors and sonicated (2 s pulse/2 s pause×5, 20% amplitude). The homogenate is centrifuged for 10 min at 20,000g at 4℃. The cell extract(0.2 mg/ml, 50 μl/well) is coated in the wells of a 96-well microtiter plate for 12 h at 4℃. The wells are then overcoated with 5% BSA in PBS for 1 h at room temperature. After washing three times with PBST, BP incorporated into the cellular proteins is assessed as performed in microtiter plate assays.[1] |
细胞实验 | Animal Models: wild-type (Wt) and R6/2 mice; Dosages: 112, 225, and 400 mg/kg; Administration: i.p.[2] |
数据来源文献 | [1] Jeon JH, et al. Exp Mol Med. 2004, 36(6):576-81. [2] Dedeoglu A, et al. J Neurosci. 2002, 22(20):8942-50. |
规格 | 50mg 100mg |
是CYP2C9的特异性抑制剂。
吡唑蒽酮 标准品
EC | EINECS 204-955-6 |
MDL | MFCD00022289 |
别名 | 1,9-吡唑并蒽酮;蒽并吡唑酮 |
英文名称 | 1,9-Pyrazoloanthrone |
CAS | 129-56-6 |
分子式 | C14H8N2O |
分子量 | 220.23 |
储存条件 | 2-8℃ |
纯度 | HPLC≥98% |
单位 | 瓶 |
SMILES | O=C1C2=C3C(NN=C3C4=C1C=CC=C4)=CC=C2 |
规格 | 20mg |
安乃近 标准品
英文名称 | Analgin |
CAS | 5907-38-0 |
分子式 | C13H16N3O4S.Na |
分子量 | 333.34 |
储存条件 | 2-8℃ |
规格 | 200mg |
吡唑蒽酮
EC | EINECS 204-955-6 |
MDL | MFCD00022289 |
InChIKey | ACPOUJIDANTYHO-UHFFFAOYSA-N |
InChI | InChI=1S/C14H8N2O/c17-14-9-5-2-1-4-8(9)13-12-10(14)6-3-7-11(12)15-16-13/h1-7H,(H,15,16) |
PubChem CID | 8515 |
别名 | 1,9-吡唑并蒽酮;吡唑蒽酮 |
英文名称 | SP600125 |
CAS | 129-56-6 |
分子式 | C14H8N2O |
分子量 | 220.23 |
纯度 | Purity≥98% |
单位 | 支 |
生物活性 | SP600125是一种可逆,ATP竞争性的 JNK 抑制剂,抑制 JNK1, JNK2 和 JNK3 的 IC50 分别为 40, 40, 90 nM。[1-5] |
In Vitro | 在小鼠β细胞中,MIN6,SP600125(20μM)诱导p38 MAPK的磷酸化及其下游CREB依赖性启动子激活[2]。在HCT116细胞中,SP600125(20μM)阻断G2期至有丝分裂转变并诱导核内复制。 SP600125的这种能力与JNK抑制无关,但由于其抑制Aurora A和Polo样激酶1上游的CDK1-细胞周期蛋白B激活[3]。SP600125是一种ATP竞争性JNK2抑制剂,Ki值为0.19±0.06μM。SP600125抑制c-Jun的磷酸化,在Jurkat T细胞中IC50为5μM至10μM。在CD4 +细胞中,例如从人脐带或外周血中分离的Th0细胞,SP600125阻断细胞活化和分化,并抑制炎症基因COX-2,IL-2,IL-10,IFN-γ和TNF-α的表达。 ,IC50为5μM至12μM[1]。 |
In Vivo | 以15或30mg/kg静脉内施用SP600125显著抑制TNF-α血清水平,而口服施用剂量依赖性地阻断TNF-α表达,在口服30mg/kg时观察到显著抑制[1]。 SP600125在体内减轻LPS诱导的大鼠ALI。 SP600125组大鼠BALF中TNF-α和IL-6的表达水平显著降低[4]。 |
SMILES | O=C1C2=C3C(NN=C3C4=C1C=CC=C4)=CC=C2 |
靶点 | Ferroptosis;JNK |
动物实验 | 小鼠[1]雌性CD-1小鼠(8-10周龄)在PPCES载体中静脉注射或口服SP600125(30%PEG-400/20%聚丙二醇/ 15%Cremophor EL/5%乙醇/ 30%)在用盐水(0.5mg/kg)中的LPS静脉注射之前15分钟,最终体积为5mL/kg。在90分钟时,从腹腔静脉获得末端出血,并回收血清。通过使用ELISA分析样品的小鼠TNF-α。大鼠[4]将40只雄性Wistar大鼠随机分为4组(n = 10):对照组,LPS组,生理盐水组(NS)和SP600125组。通过气管内注射LPS诱导急性肺损伤(ALI)。简而言之,用戊巴比妥钠麻醉大鼠,然后气管内注射5mg/kg LPS。然后将大鼠置于垂直位置并旋转1分钟以将LPS分布在肺中。在LPS注射后10分钟通过腹膜内注射(15mg/kg)给予生理盐水或SP600125。 |
细胞实验 | 基本上进行mRNA半衰期的测定,除了在加入放线菌素D(5μg/ mL)之前用(细菌)脂多糖(LPS; 50ng/mL)刺激CD14 +细胞2小时。在放线菌素D之后立即加入SP600125(25μM)或载体(0.5%DMSO vol/vol)。通过使用实时逆转录(RT)-PCR进行分析。用RNeasy Mini试剂盒提取总RNA。使用TNF Taqman探针通过实时RT-PCR测量TNF mRNA。通过使用甘油醛-3-磷酸脱氢酶(GAPDH)表达将所有数据标准化。 TNF-α正向引物是5-CTGGCCCAGGCAGTCAGAT-3,反向引物是5-TATCTCTCAGCTCCACGCCATT-3。 Taqman探针序列是5-FAM-CCTGTAGCCCATGTTGTAGCAAACCCTCA-TAMRA-3[1]。 |
数据来源文献 | [1]. Bennett BL, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686. [2]. Vaishnav D, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochem Biophys Res Commun, 2003, 307(4), 855-860. [3]. Kim JA, et al. SP600125 suppresses Cdk1 and induces endoreplication directly from G2 phase, independent of JNK inhibition. Oncogene, 2010, 29(11), 1702-1716. [4]. Zheng Y, et al. JNK inhibitor SP600125 protects against lipopolysaccharide-induced acute lung injury via upregulation ofclaudin-4. Exp Ther Med. 2014 Jul;8(1):153-158. [5]. Zhang H, et al. SP600125 Suppresses Keap1 Expression and Results in NRF2-mediated Prevention of Diabetic Nephropathy. J Mol Endocrinol. J Mol Endocrinol. 2018 Feb;60(2):145-157. |
规格 | 10mg 10mM*1mL in DMSO 50mg |
SP600125是一种可逆,ATP竞争性的 JNK 抑制剂。