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TAK-220

NMR下載 COA and HPLC MSDS下載
names：
TAK-220
CAS號：
333994-00-6
MDL Number： MFCD28502079
MF(分子式)： C31H41ClN4O3 MW(分子量)： 553.14
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

TAK-220(333994-00-6)是口服可生物利用的小分子CCR5拮抗劑。目標(biāo)：CCR； TAK-220是新型趨化因子受體拮抗劑的成員，對CCR5具有高度特異性。TAK-220抑制RANTES與表達CCR5的細(xì)胞結(jié)合，IC50為3.5 nM，而它抑制膜融合和病毒復(fù)制，EC50分別為0.42 nM和0.60至0.68 nM。TAK-220抑制R5 HIV-1（JR-FL）包膜介導(dǎo)的膜融合，IC50值為0.42 nM，但不影響X4 HIV-1（HXB2）包膜介導(dǎo)的膜融合，即使在濃度為1,000 nM。

貨品編碼	規(guī)格	純度	價格 (￥)	現(xiàn)價(￥)	特價(￥)	庫存描述	數(shù)量	總計 (￥)
YZM000650-5mg	5mg	99.95%	￥ 3543.00	￥ 3543.00		2-3天	- +	￥ 0.00
YZM000650-1mg	1mg	99.95%	￥ 1462.50	￥ 1462.50		2-3天	- +	￥ 0.00

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中文別名	TAK-220(333994-00-6), TAK-220，TAK 220，TAK220; 1-乙酰基-N- [3- [4-[（4-氨基甲?；交┘谆鵠哌啶-1-基]丙基] -N-（3-氯-4-甲基苯基）哌啶-4-羧酰胺;
英文別名	TAK-220(333994-00-6), TAK-220, TAK 220, TAK220; 1-acetyl-N-[3-[4-[(4-carbamoylphenyl)methyl]piperidin-1-yl]propyl]-N-(3-chloro-4-methylphenyl)piperidine-4-carboxamide;
CAS號	333994-00-6
Inchi	InChI=1S/C31H41ClN4O3/c1-22-4-9-28(21-29(22)32)36(31(39)27-12-18-35(19-13-27)23(2)37)15-3-14-34-16-10-25(11-17-34)20-24-5-7-26(8-6-24)30(33)38/h4-9,21,25,27H,3,10-20H2,1-2H3,(H2,33,38)
InchiKey	ASSJTMUEFHUKMJ-UHFFFAOYSA-N
分子式 Formula	C31H41ClN4O3
分子量 Molecular Weight	553.14
溶解度Solubility	生物體外In Vitro:DMSO溶解度≥ 50 mg/mL(90.39 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性狀	固體粉末,Power
儲藏條件 Storage conditions	-20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月

TAK-220(333994-00-6)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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產(chǎn)品說明	TAK-220(333994-00-6)是口服生物利用小分子CCR5拮抗劑。
Introduction	TAK20is a selective and orally bioavailableCCR5antagonist, withIC50s of 3.5nM and1.4nM for inhibition on the binding of RANTES and MIPα to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK20 also selectively inhibitsHIV, withEC50s of 1.2nM (HIVKK)0.72nM(HIVCTV)1.7nM(HIVHKW)1.7nM(HIVHNK)0.93nM(HIV HTN)and0.55nM(HIV HHA)andEC90s of 12 nM(HIV KK)5nM(HIV CTV)12nM(HIV HKW)28nM(HIV HNK)15nM(HIV HTN)and4nM(HIV HHA)in PBMCs.
Application1	TAK-220(333994-00-6)是口服生物利用小分子CCR5拮抗劑。TAK-220是GPCR / G蛋白；可用于免疫學(xué)的炎癥。
Application2	(333994-00-6)TAK-220 是一種有效的選擇性的可口服的CCR5拮抗劑夠抑制 RANTES，MIP-1α 與 CCR5 結(jié)合，IC50值分別是 3.5 nM 和 1.4 nM，但是對 CCR1，CCR2b，CCR3，CCR4 或者 CCR7 無作用; TAK-220 也可選擇性地抑制HIV-1，在外周單核細(xì)胞中，EC50值分別是 1.2 nM (HIV-1 KK)，0.72 nM (
Application3	0.72 nM (HIV-1 CTV)，1.7 nM (HIV-1 HKW)，1.7 nM (HIV-1 HNK)，0.93 nM (HIV-1 HTN) 和 0.55 nM (HIV-1 HHA)，EC90值分別是 12 nM (HIV-1 KK)，5 nM (HIV-1 CTV)，12 nM (HIV-1 HKW)，28 nM (HIV-1 HNK)，15 nM (HIV-1 HTN) 及 4

TAK-220(333994-00-6)藥理學(xué)：

※TAK-220是GPCR / G蛋白；可用于免疫學(xué)的炎癥。

※TAK-220是口服可生物利用的小分子CCR5拮抗劑。目標(biāo)：CCR； TAK-220是新型趨化因子受體拮抗劑的成員，對CCR5具有高度特異性。TAK-220抑制RANTES與表達CCR5的細(xì)胞結(jié)合，IC50為3.5 nM，而它抑制膜融合和病毒復(fù)制，EC50分別為0.42 nM和0.60至0.68 nM。TAK-220抑制R5 HIV-1（JR-FL）包膜介導(dǎo)的膜融合，IC50值為0.42 nM，但不影響X4 HIV-1（HXB2）包膜介導(dǎo)的膜融合，即使在濃度為1,000 nM。

※TAK-220是一種選擇性CCR5拮抗劑，具有IC₅₀3.5 nM和1.4 nM分別抑制CHO細(xì)胞中RANTES和MIP-1α與CCR5的結(jié)合，但對CCR1，CCR2b，CCR3，CCR4或CCR7的結(jié)合沒有影響。TAK-220（0-1000 nM）與CCR5相互作用，但與RANTES不相互作用，并抑制CCR5介導(dǎo)的Casup> 2+信號傳導(dǎo)。TAK-220通過IC抑制R5 HIV-1（JR-FL）包膜介導(dǎo)的膜融合₅₀值為0.42 nM，但不會改變X4 HIV-1（HXB2）包膜介導(dǎo)的膜融合。TAK-220還可以通過EC選擇性抑制HIV-1₅₀分別為1.2 nM（HIV-1 KK），0.72 nM（HIV-1 CTV），1.7 nM（HIV-1 HKW），1.7 nM（HIV-1 HNK），0.93 nM（HIV-1 HTN）和0.55 nM （HIV-1 HHA）和EC₉₀12 nM（HIV-1 KK），5 nM（HIV-1 CTV），12 nM（HIV-1 HKW），28 nM（HIV-1 HNK），15 nM（HIV-1 HTN）和4 nM PBMC中的（HIV-1 HHA）。TAK-220對R5分離物具有強抑制活性，具有IC₅₀抗HIV-1 R5-08的濃度為3.12 nM，抗HIV-1 R5-06的濃度為13.47 nM，抗HIV-1 R5-18的濃度為2.26 nM。TAK-220（> 100 nM）對未感染的PBMC無毒性。

警示圖
危險性	warning
危險性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害
安全防護	P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護理
備注	實驗過程中防止吸入、食入，做好安全防護

Takashima K, et al. Highly potent inhibition of human immunodeficiency virus type 1 replication by TAK-220, an orally bioavailable small-molecule CCR5 antagonist. Antimicrob Agents Chemother. 2005 Aug

Tremblay CL, et al. TAK-220, a novel small-molecule CCR5 antagonist, has favorable anti-human immunodeficiency virus interactions with other antiretrovirals in vitro. Antimicrob Agents Chemother. 2005

Binding site exploration of CCR5 using in silico methodologies: a 3D-QSAR approach Archives of Pharmacal Research 2013 23325486

Selective and Dual Targeting of CCR2 and CCR5 Receptors: A Current Overview Chemokines 2014

What’s New in HIV/AIDS? Chemokine Receptor Antagonists: A New Era of HIV Therapy? Infection 2005 16258879

TAK-220(333994-00-6)參考文獻：

1.New advances in HIV entry inhibitors development.
Rusconi S;Scozzafava A;Mastrolorenzo A;Supuran CT Curr Drug Targets Infect Disord. 2004 Dec;4(4):339-55.

Considerable advances have been made in the last years in the design of derivatives acting as inhibitors of HIV entry and fusion. The discovery of chemokines focused the attention on cellular coreceptors used by the virus for entering within cells, and consequently the various steps of such processes have been characterized in detail. Intense research led to a wide range of effective compounds that are able to inhibit the initial steps of HIV life cycle. All steps in the process of HIV entry into the cell may be targeted by specific compounds that may be developed as novel types of antiretrovirals. Thus, several inhibitors of the gp120-CD4 interaction have been detected so far (zintevir, FP-21399 and BMS-378806 in clinical trials). Small molecule chemokine receptor antagonists acting as HIV entry inhibitors also were described in the last period, which interact both with the CXCR4 coreceptor (such as AMD3100; AMD3465; ALX40-4C; T22, T134 and T140), or which are antagonist of the CCR5 coreceptor (TAK-779, TAK-220, SCH-C, SCH-D, E913, AK-602, UK-427857 and NSC 651016 in clinical trials), together with new types of fusion inhibitors possessing the same mechanism of action as enfuvirtide (such as T1249).

2.Analysis of binding sites for the new small-molecule CCR5 antagonist TAK-220 on human CCR5.
Nishikawa M;Takashima K;Nishi T;Furuta RA;Kanzaki N;Yamamoto Y;Fujisawa J Antimicrob Agents Chemother. 2005 Nov;49(11):4708-15.

G protein-coupled receptor CCR5 is the main coreceptor for macrophage-tropic human immunodeficiency virus type 1 (HIV-1), and various small-molecule CCR5 antagonists are being developed to treat HIV-1 infection. It has been reported that such CCR5 antagonists, including TAK-779, bind to a putative binding pocket formed by transmembrane domains (TMs) 1, 2, 3 and 7 of CCR5, indicating the importance of the conformational changes of the TMs during virus entry. In this report, using a single-round infection assay with human CCR5 and its substitution mutants, we demonstrated that a new CCR5 antagonist, TAK-220, shares the putative interacting amino acid residues Asn252 and Leu255 in TM6 with TAK-779 but also requires the distinct residues Gly163 and Ile198 in TMs 4 and 5, respectively, for its inhibitory effect. We suggested that, together with molecular models of the interactions between the drugs and CCR5, the inhibitory activity of TAK-220 could involve direct interactions with amino acid residues in TMs 4, 5, and 6 in addition to those in the previously postulated binding pocket. The possible interaction of drugs with additional regions of the CCR5 molecule would help to develop a new small-molecule CCR5 antagonist.

3.Discovery of a piperidine-4-carboxamide CCR5 antagonist (TAK-220) with highly potent Anti-HIV-1 activity.
Imamura S;Ichikawa T;Nishikawa Y;Kanzaki N;Takashima K;Niwa S;Iizawa Y;Baba M;Sugihara Y J Med Chem. 2006 May 4;49(9):2784-93.

We incorporated various polar groups into previously described piperidine-4-carboxamide CCR5 antagonists to improve their metabolic stability in human hepatic microsomes. Introducing a carbamoyl group into the phenyl ring of the 4-benzylpiperidine moiety afforded the less lipophilic compound 5f, which possessed both high metabolic stability and good inhibitory activity of HIV-1 envelope-mediated membrane fusion (IC(50) = 5.8 nM). Further optimization to increase potency led to the discovery of 1-acetyl-N-{3-[4-(4-carbamoylbenzyl)piperidin-1-yl]propyl}-N-(3-chloro-4-methylphenyl)piperidine-4-carboxamide (5m, TAK-220), which showed high CCR5 binding affinity (IC(50) = 3.5 nM) and potent inhibition of membrane fusion (IC(50) = 0.42 nM), as well as good metabolic stability. Compound 5m strongly inhibited the replication of CCR5-using HIV-1 clinical isolates in human peripheral blood mononuclear cells (mean EC(50) = 1.1 nM, EC(90) = 13 nM) and exhibited a good pharmacokinetic profile in monkeys (BA = 29%). This compound has been chosen as a clinical candidate for further development.

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