3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂 102052-95-9_详细资料

产品信息

货号： A 1905 保存条件： -20 供应商：上海恒斐生物科技有限公司 CAS号： 102052-95-9 英文名： 3-Deazaneplanocin,DZNep 数量：现货规格： 1mg

3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂 102052-95-93-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂化学性质

CAS号 102052-95-9 SDF Download SDF

别名 DZNep, 3-Deazaneplanocin A,NSC 617989,NSC617989

化学名 (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol

SMILES C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N

分子式 C₁₂H₂₄N₄O₃ 分子量 262.26

溶解性 Soluble in Water 储存条件 Store at -20°C

物理性状 A crystalline solid 运输条件 SY装：蓝冰运输。
其他可选规格：常温运输或根据您的要求用蓝冰运输。

一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。

3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂生物活性

描述 3-deazaneplanocin A (DZNeP)，腺苷类似物，是S-腺苷高半胱氨酸水解酶（S-adenosylhomocysteine hydrolase）的竞争性YZ剂，Ki值为50 pM。

靶点 S-adenosylhomocysteine hydrolase

IC50 50 pM (K_i)

3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂实验操作

细胞实验[1]：

细胞系

人急性性白血病（AML）细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

100-750 nM；24-72 h

应用

在培养的和原代AML细胞中，DZNep诱导细胞凋亡。在AML HL-60和OCI-AML3细胞中，DZNep耗尽EZH2水平，YZ组蛋白H3赖氨酸27（H3K27）的三甲基化。在cyclin E和HOXA9水平耗尽之后，DZNep诱导p16、p21、p27和FBXO32的水平。

动物实验[2]：

动物模型

Sprague-Dawley大鼠（120-140 g）

剂量

5 μM；实验前24小时处理，随饮食口服。

应用

在非酒精性脂肪性肝病（NAFLD）小鼠模型中，DZNep显著减少EZH2的表达和活性，增加脂质沉积、炎症分子和microRNAs。

注意事项

请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。

References:

1. Fiskus W1, Wang Y, Sreekumar A et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells. Blood. 2009 Sep 24;114(13):2733-43.

2. Vella S, Gnani D, Crudele A et al. EZH2 down-regulation exacerbates lipid accumulation and inflammation in vitro and in vivo NAFLD.Int J Mol Sci. 2013 Dec 12;14(12):24154-68.
3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂研究更新
1. Cell-based proteome profiling using an affinity-based probe (AfBP) derived from 3-deazaneplanocin A (DzNep). Chem Asian J. 2013 Aug;8(8):1818-28. doi: 10.1002/asia.201300303. Epub 2013 Jun 7.
Abstract
A novel probe derived from DzNep, an inhibitor of histone methylation, was used to identify potential cellular targets of DzNep in living mammalian cells.
2. 3-Deazaneplanocin A (DZNep), an inhibitor of S-adenosyl-methionine-dependent methyltransferase, promotes erythroid differentiation. J Biol Chem. 2014 Feb 3. [Epub ahead of print]
Abstract
DZNep significantly induced erythroid differentiation in K562 cells and human primary erythroblasts derived from cord blood CD34-positive cells and reduced levels of ETO2 protein in K562 cells, which indicates DZNep induced erythroid differentiation may be partially attributed to its inhibition of ETO2 rather than EZH2 inhibition.
3. PRIMA-1, a Mutant p53 Reactivator, Restores the Sensitivity of TP53 Mutant-type Thyroid Cancer Cells to the Histone Methylation Inhibitor 3-Deazaneplanocin A (DZNep). J Clin Endocrinol Metab. 2014 Feb 10:jc20133147. [Epub ahead of print]
Abstract
DZNep inhibited the growth of TP53 wild-type cells by promoting p53 protein accumulation and activating p53 pathways and failed to inhibit the growth of TP53 mutant-type cells, even though DZNep induced EZH2 depletion and H3K27me3 histone mark reduction were observed in both thyroid cancer cells. However, the combination of DZNep/PRIMA-1 restored the sensitivity of TP53 mutant-type cells to DZNep by reactivating p53.
4. TP53 genomic status regulates sensitivity of gastric cancer cells to the histone methylation inhibitor 3-deazaneplanocin A (DZNep). Clin Cancer Res. 2012 Aug 1;18(15):4201-12. doi: 10.1158/1078-0432.CCR-12-0036. Epub 2012 Jun 6.
Abstract
DZNep exhibits its anticancer activity by depleting EZH2.
5. Epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A inhibits the growth of cholangiocarcinoma cells. Oncol Rep. 2014 Feb;31(2):983-8. doi: 10.3892/or.2013.2922. Epub 2013 Dec 13.
Abstract
DZNep depleted EZH2, inhibited histone lysine 27 trimethylation and suppressed proliferation partially through upregulation of p16INK4a and p17KIP1 in cholangiocarcinoma cell lines RBE and TFK-1 resulting in induced G1 arrest and apoptosis. 3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂产品描述
3- Deazaneplanocin是一种GX的S-腺苷高半胱氨酸水解酶YZ剂，Ki值为0.05 nM[1]。

3- Deazaneplanocin是腺苷的类似物，与底物腺苷竞争YZS-腺苷高半胱氨酸水解酶。3-Deazaneplanocin对细胞生长的YZ作用较弱。在HL-60细胞中，10 μM的3-Deazaneplanocin处理只能适度减少细胞的生长。在HCC肝癌细胞系Huh1和Huh7中，3-Deazaneplanocin剂量依赖性地YZ细胞的生长和非粘附球的形成。在Huh1细胞中，3-Deazaneplanocin将上皮细胞粘附分子EpCAM从49.0％减少到12.5%。在Huh7细胞中，3-Deazaneplanocin将EpCAM从44.4%减少到11.6%。在异种移植Huh7细胞的小鼠中，3-Deazaneplanocin通过直接影响肿瘤起始细胞的生长和自我更新，从而YZ肿瘤的发生和生长[1, 2]。

3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂参考文献：
[1] Glazer R I, Hartman K D, Knode M C, et al. 3-Deazaneplanocin: a new and potent inhibitor of S-adenosylhomocysteine hydrolase and its effects on human promyelocytic leukemia cell line HL-60. Biochemical and biophysical research communications, 1986, 135(2): 688-694.
[2] Chiba T, Suzuki E, Negishi M, et al. 3-Deazaneplanocin A is a promising therapeutic agent for the eradication of tumor-initiating hepatocellular carcinoma cells. International Journal of Cancer, 2012, 130(11): 2557-2567.
3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂上海恒斐生物现货供应说明书及YZ剂详情请联系上海恒斐生物021-60493872 刘鑫 17317793691（微信同步）QQ845206284
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CAS号	102052-95-9	SDF	Download SDF
别名	DZNep, 3-Deazaneplanocin A,NSC 617989,NSC617989
化学名	(1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol
SMILES	C1=CN=C(C2=C1N(C=N2)C3C=C(C(C3O)O)CO)N
分子式	C₁₂H₂₄N₄O₃	分子量	262.26
溶解性	Soluble in Water	储存条件	Store at -20°C
物理性状	A crystalline solid	运输条件	SY装：蓝冰运输。其他可选规格：常温运输或根据您的要求用蓝冰运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。

描述	3-deazaneplanocin A (DZNeP)，腺苷类似物，是S-腺苷高半胱氨酸水解酶（S-adenosylhomocysteine hydrolase）的竞争性YZ剂，Ki值为50 pM。
靶点	S-adenosylhomocysteine hydrolase
IC50	50 pM (K_i)

细胞实验[1]：
细胞系	人急性性白血病（AML）细胞
溶解方法	在DMSO中的溶解度>10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。
反应条件	100-750 nM；24-72 h
应用	在培养的和原代AML细胞中，DZNep诱导细胞凋亡。在AML HL-60和OCI-AML3细胞中，DZNep耗尽EZH2水平，YZ组蛋白H3赖氨酸27（H3K27）的三甲基化。在cyclin E和HOXA9水平耗尽之后，DZNep诱导p16、p21、p27和FBXO32的水平。
动物实验[2]：
动物模型	Sprague-Dawley大鼠（120-140 g）
剂量	5 μM；实验前24小时处理，随饮食口服。
应用	在非酒精性脂肪性肝病（NAFLD）小鼠模型中，DZNep显著减少EZH2的表达和活性，增加脂质沉积、炎症分子和microRNAs。
注意事项	请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。
References: 1. Fiskus W1, Wang Y, Sreekumar A et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells. Blood. 2009 Sep 24;114(13):2733-43. 2. Vella S, Gnani D, Crudele A et al. EZH2 down-regulation exacerbates lipid accumulation and inflammation in vitro and in vivo NAFLD.Int J Mol Sci. 2013 Dec 12;14(12):24154-68. 3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂研究更新 1. Cell-based proteome profiling using an affinity-based probe (AfBP) derived from 3-deazaneplanocin A (DzNep). Chem Asian J. 2013 Aug;8(8):1818-28. doi: 10.1002/asia.201300303. Epub 2013 Jun 7. Abstract A novel probe derived from DzNep, an inhibitor of histone methylation, was used to identify potential cellular targets of DzNep in living mammalian cells. 2. 3-Deazaneplanocin A (DZNep), an inhibitor of S-adenosyl-methionine-dependent methyltransferase, promotes erythroid differentiation. J Biol Chem. 2014 Feb 3. [Epub ahead of print] Abstract DZNep significantly induced erythroid differentiation in K562 cells and human primary erythroblasts derived from cord blood CD34-positive cells and reduced levels of ETO2 protein in K562 cells, which indicates DZNep induced erythroid differentiation may be partially attributed to its inhibition of ETO2 rather than EZH2 inhibition. 3. PRIMA-1, a Mutant p53 Reactivator, Restores the Sensitivity of TP53 Mutant-type Thyroid Cancer Cells to the Histone Methylation Inhibitor 3-Deazaneplanocin A (DZNep). J Clin Endocrinol Metab. 2014 Feb 10:jc20133147. [Epub ahead of print] Abstract DZNep inhibited the growth of TP53 wild-type cells by promoting p53 protein accumulation and activating p53 pathways and failed to inhibit the growth of TP53 mutant-type cells, even though DZNep induced EZH2 depletion and H3K27me3 histone mark reduction were observed in both thyroid cancer cells. However, the combination of DZNep/PRIMA-1 restored the sensitivity of TP53 mutant-type cells to DZNep by reactivating p53. 4. TP53 genomic status regulates sensitivity of gastric cancer cells to the histone methylation inhibitor 3-deazaneplanocin A (DZNep). Clin Cancer Res. 2012 Aug 1;18(15):4201-12. doi: 10.1158/1078-0432.CCR-12-0036. Epub 2012 Jun 6. Abstract DZNep exhibits its anticancer activity by depleting EZH2. 5. Epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A inhibits the growth of cholangiocarcinoma cells. Oncol Rep. 2014 Feb;31(2):983-8. doi: 10.3892/or.2013.2922. Epub 2013 Dec 13. Abstract DZNep depleted EZH2, inhibited histone lysine 27 trimethylation and suppressed proliferation partially through upregulation of p16INK4a and p17KIP1 in cholangiocarcinoma cell lines RBE and TFK-1 resulting in induced G1 arrest and apoptosis. 3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂产品描述 3- Deazaneplanocin是一种GX的S-腺苷高半胱氨酸水解酶YZ剂，Ki值为0.05 nM[1]。 3- Deazaneplanocin是腺苷的类似物，与底物腺苷竞争YZS-腺苷高半胱氨酸水解酶。3-Deazaneplanocin对细胞生长的YZ作用较弱。在HL-60细胞中，10 μM的3-Deazaneplanocin处理只能适度减少细胞的生长。在HCC肝癌细胞系Huh1和Huh7中，3-Deazaneplanocin剂量依赖性地YZ细胞的生长和非粘附球的形成。在Huh1细胞中，3-Deazaneplanocin将上皮细胞粘附分子EpCAM从49.0％减少到12.5%。在Huh7细胞中，3-Deazaneplanocin将EpCAM从44.4%减少到11.6%。在异种移植Huh7细胞的小鼠中，3-Deazaneplanocin通过直接影响肿瘤起始细胞的生长和自我更新，从而YZ肿瘤的发生和生长[1, 2]。 3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂参考文献： [1] Glazer R I, Hartman K D, Knode M C, et al. 3-Deazaneplanocin: a new and potent inhibitor of S-adenosylhomocysteine hydrolase and its effects on human promyelocytic leukemia cell line HL-60. Biochemical and biophysical research communications, 1986, 135(2): 688-694. [2] Chiba T, Suzuki E, Negishi M, et al. 3-Deazaneplanocin A is a promising therapeutic agent for the eradication of tumor-initiating hepatocellular carcinoma cells. International Journal of Cancer, 2012, 130(11): 2557-2567. 3-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂上海恒斐生物现货供应说明书及YZ剂详情请联系上海恒斐生物021-60493872 刘鑫 17317793691（微信同步）QQ845206284 进口YZ剂相关产品 B1577C646HAT p300-CBPYZ剂 C5773CTPB组蛋白乙酰转移酶（HAT）p300的选择性激活剂 C5000HAT Inhibitor II组蛋白乙酰转移酶p300的YZ剂 C3209Butyrolactone 3组蛋白乙酰转移酶Gcn5YZ剂 C3208CPTH2 (hydrochloride)Gcn5的HAT活性YZ剂 A8712MCB-613类固醇受体共激活因子（SRC）刺激物 B4946GarcinolPCAF和p300组蛋白乙酰转移酶（HAT）活性YZ剂 B4945IWP 12PORCNYZ剂 B4887RemodelinNAT10YZ剂 B7739L002p300YZ剂 B7679(R)-(+)-Etomoxir sodium salt肉碱棕榈酰转移酶I（CPT1）YZ剂 B7250YM 750酰基辅酶A：胆固醇酰基转移酶（ACAT）YZ剂 B7241VULM 1457酰基辅酶A：胆固醇酰基转移酶（ACAT）YZ剂 B6987CI 976酰基辅酶A：胆固醇酰基转移酶（ACAT）YZ剂 A4492NU 9056KAT5（Tip60）HATYZ剂 B1602Donepezil HClAChEYZ剂 A4190GSK J4 HClH3K27去甲基化酶JMJD3的YZ剂 B6084AS8351组蛋白去甲基化酶YZ剂 B7811CPI-455KDM5YZ剂 C3584PBITJARID1家族去甲基化酶YZ剂 C3630Lysine-specific Demethylase Inhibitor (1C)赖氨酸特异性去甲基化酶YZ剂 C3095N-Oxalylglycineα-酮戊二酸依赖性酶（包括JMJD2A，JMJD2C和JMJD2E）的细胞渗透性YZ剂 C4247RN-1 (hydrochloride)LSD1YZ剂 C4202GSK-LSD1 (hydrochloride)LSD1YZ剂 C5162BizineLSD1YZ剂 A8766OG-L002 HClLSD1YZ剂 B5959GSK J4 free base组蛋白去甲基化酶JMJD3/UTXYZ剂 B59722,4-Pyridinedicarboxylic Acid组蛋白LSDYZ剂 B7514Tranylcypromine hydrochloride单胺氧化酶YZ剂 B5607IOX 1组蛋白去甲基化酶JMJDYZ剂 B5685GSK J2GSK J1（JMJD3（KDM6B）和UTX（KDM6A）YZ剂）的无活性对照 B5686GSK J5GSK J4（KDMYZ剂）的无活性异构体 B5784RN 1 dihydrochlorideLSD1YZ剂 B4891ML324JMJD2去甲基化酶YZ剂 B4894SP2509新型LSD1拮抗剂 B4930TC-E 5002选择性组蛋白去甲基化酶KDM2/7亚家族YZ剂 B4983GSK-LSD1 2HClLSD1YZ剂 B5879GSK2879552LSD1YZ剂 B1578Tranylcypromine (2-PCPA) HClNew Product, Cas No.:4548-34-9, Please Inquiry B1580OG-L002LSD1YZ剂 B1263CBB1007LSD1YZ剂 A4191GSK J1H3K27去甲基化酶JMJD3YZ剂 A4171EPZ005687 EZH2YZ剂 A4168EntacaponeCOMTYZ剂 A4166EPZ5676DOT1LYZ剂 A19053-Deazaneplanocin,DZNep S-腺苷高半胱氨酸和EZH2YZ剂。 A1146Histone-H2A-(107-122)-Ac-OH组蛋白H2A肽 B608MI5/Eosin Y disodium salt蛋白甲基转移酶YZ剂/伊红，用于苏木@精伊红染色(HE染色) B6088EPZ020411PRMT6YZ剂 B6119LLY507SMYD2YZ剂 B6120Adox间接甲基转移酶YZ剂 B6168OICR-9429Wdr5-MLL相互作用拮抗剂 B6182GSK591PRMT5YZ剂 B6183MS023I型PRMTsYZ剂 B7806HLCL-61PRMT5YZ剂 B7819CPI-1205EZH2YZ剂 C3503MS023 (hydrochloride)I型PRMTsYZ剂 C3776MS049 (hydrochloride)PRMT4和PRMT6YZ剂 C4834(S)-PFI-2 (hydrochloride)(R)-PFI 2 hydrochloride的阴性对照 B8210PFI-2 (hydrochloride) B6082EPZ031686SMYD3YZ剂 B6081BAY-598SMYD2YZ剂