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催乳素

NMR下載 COA and HPLC MSDS下載
names：
Brilacidin
CAS號(hào)：
1224095-98-0
MDL Number： MFCD23726663
MF(分子式)： C40H50F6N14O6 MW(分子量)： 936.91
EINECS: Reaxys Number:
Pubchem ID:25023695 Brand:BIOFOUNT

催乳素(Brilacidin,PMX 30063,1224095-98-0)是一種抗菌劑，對革蘭氏陽性菌肺炎鏈球菌和綠色鏈球菌的MIC90分別為1和8μg/ mL，對革蘭氏陰性菌流感嗜血桿菌和銅綠假單胞菌的MIC90分別為8和4μg/ mL。溴酸是一種類似的防御素的抗生素（抗生素）。正在研究Brilacidin對粘膜炎，口腔炎，口腔疾病和頭頸部腫瘤的支持治療。

貨品編碼	規(guī)格	純度	價(jià)格 (￥)	現(xiàn)價(jià)(￥)	特價(jià)(￥)	庫存描述	數(shù)量	總計(jì) (￥)
YZM000175-1mg	1mg	>97%	￥ 9945.00	￥ 9945.00		2-3天	- +	￥ 0.00

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中文別名	催乳素(1224095-98-0);布雷西丁;PMX30063;布拉菌素; PMX30063；PMX-30063；PMX 30063；4-N，6-N-雙[3- [5-（二氨基亞甲基亞氨基氨基）戊?；被鵠 -2-[（3R）-吡咯烷-3-基]氧基-5-（三氟甲基）苯基]嘧啶-4,6-二甲酰胺;
英文別名	Brilacidin(1224095-98-0);brilacidin;PMX30063;N,N'-Bis(3-((5-(carbamimidoylamino)pentanoyl)amino)-2-((3R)-pyrrolidin-3-yloxy)-5-(trifluoromethyl)phenyl)pyrimidine-4,6-dicarboxamide; 4,6-Pyrimidinedicarboxamide,N4,N6-bis(3-((5-((aminoiminomethyl)amino)-1-oxopentyl)amino)-2-((3R)-3-pyrrolidinyloxy)-5-(trifluoromethyl)phenyl); Brilacidin (USAN); 4-N,6-N-bis[3-[5-(diaminomethylideneamino)pentanoylamino]-2-[(3R)-pyrrolidin-3-yl]oxy-5-(trifluoromethyl)phenyl]pyrimidine-4,6-dicarboxamide;
CAS號(hào)	1224095-98-0
Inchi	InChI=1S/C40H50F6N14O6/c41-39(42,43)21-13-25(57-31(61)5-1-3-9-53-37(47)48)33(65-23-7-11-51-18-23)27(15-21)59-35(63)29-17-30(56-20-55-29)36(64)60-28-16-22(40(44,45)46)14-26(34(28)66-24-8-12-52-19-24)58-32(62)6-2-4-10-54-38(49)50/h13-17,20,23-24,51-52H,1-12,18-19H2,(H,57,61)(H,58,62)(H,59,63)(H,60,64)(H4,47,48,53)(H4,49,50,54)/t23-,24-/m1/s1
InchiKey	QPDYBCZNGUJZDK-DNQXCXABSA-N
分子式 Formula	C40H50F6N14O6
分子量 Molecular Weight	936.91
溶解度Solubility
性狀	固體粉末,Power
儲(chǔ)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

催乳素(Brilacidin,PMX 30063,1224095-98-0)實(shí)驗(yàn)注意事項(xiàng)：
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡，穿戴防護(hù)服和口罩，佩戴手套，避免與皮膚接觸。
2.實(shí)驗(yàn)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(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類存儲(chǔ)，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.

Tags:催乳素試劑催乳素雜質(zhì),催乳素合成,催乳素中間體,催乳素密度,催乳素溶解度,催乳素旋光度,催乳素閃點(diǎn),催乳素熔點(diǎn),催乳素購買,

產(chǎn)品說明	催乳素(Brilacidin,PMX 30063,1224095-98-0)是一種新型的防御素模擬物中的非肽類抗感染藥,正在開發(fā)用于治療眼部感染。
Introduction	催乳素(Brilacidin,PMX 30063,1224095-98-0) is a nonpeptidic antinfective in a new class of defensin mimetics that is being developed for the treatment of eye infections.
Application1
Application2
Application3

催乳素(Brilacidin,PMX 30063,1224095-98-0)藥理學(xué)：

一種對革蘭氏陽性和革蘭氏陰性細(xì)菌有效的研究性抗生素，這是一種以宿主防御肽（HDP）為模型的非肽小分子。目前正在治療頭頸部腫瘤以及粘膜炎的臨床試驗(yàn)。

警示圖
危險(xiǎn)性	warning
危險(xiǎn)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(hù)	P264處理后徹底清洗+P280戴防護(hù)手套/穿防護(hù)服/戴防護(hù)眼罩/戴防護(hù)面具+P305如果進(jìn)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(hù)理
備注	實(shí)驗(yàn)過程中防止吸入、食入，做好安全防護(hù)

Bruk Mensa , et al. Comparative Mechanistic Studies of Brilacidin, Daptomycin, and the Antimicrobial Peptide LL16. Antimicrob Agents Chemother. 2014 Sep;58(9):5136-45.

Regis P Kowalski, et al. An Independent Evaluation of a Novel Peptide Mimetic, Brilacidin (PMX30063), for Ocular Anti-infective. J Ocul Pharmacol Ther. Jan-Feb 2016;32(1):23-7.

Comparative mechanistic studies of brilacidin, daptomycin, and the antimicrobial peptide LL16 PMID 24936592; Antimicrobial agents and chemotherapy 2014 Sep; 58(9):5136-45 Name matches: ll37 brilacidin

Mimics of Host Defense Proteins; Strategies for Translation to Therapeutic Applications PMID 27411325; Current topics in medicinal chemistry 2017; 17(5):576-589 (Review Article) Name matches: impetigo

An Independent Evaluation of a Novel Peptide Mimetic, Brilacidin (PMX30063), for Ocular Anti-infective PMID 26501484; Journal of ocular pharmacology and therapeutics : the official journal of the Asso

催乳素(Brilacidin,PMX 30063,1224095-98-0)參考文獻(xiàn)：

1.Comparative mechanistic studies of brilacidin, daptomycin, and the antimicrobial peptide LL16.
Mensa B;Howell GL;Scott R;DeGrado WF Antimicrob Agents Chemother. 2014 Sep;58(9):5136-45. doi: 10.1128/AAC.02955-14. Epub 2014 Jun 16.

Brilacidin (PMX30063) has shown potent bactericidal activity against drug-resistant and -susceptible strains of multiple Gram-negative and Gram-positive pathogens. In this study, we demonstrate that brilacidin causes membrane depolarization in the Gram-positive bacterium Staphylococcus aureus, to an extent comparable to that caused by the lipopeptidic drug daptomycin. Transcriptional profiling of Staphylococcus aureus by deep sequencing shows that the global response to brilacidin treatment is well correlated to those of treatment with daptomycin and the cationic antimicrobial peptide LL37 and mostly indicates abrogation of cell wall and membrane functions. Furthermore, the upregulation of various chaperones and proteases by brilacidin and daptomycin indicates that cytoplasmic protein misfolding stress may be a contributor to the mechanism of action of these drugs. These stress responses were orchestrated mainly by three two-component systems, GraSR, VraSR, and NsaSR, which have been implicated in virulence and drug resistance against other clinically available antibiotics.

2.An Independent Evaluation of a Novel Peptide Mimetic, Brilacidin (PMX30063), for Ocular Anti-infective.
Kowalski RP;Romanowski EG;Yates KA;Mah FS J Ocul Pharmacol Ther. 2016 Jan-Feb;32(1):23-7. doi: 10.1089/jop.2015.0098. Epub 2015 Oct 26.

OBJECTIVE: ;Brilacidin (BRI), a novel defensin mimetic, was evaluated as an ocular anti-infective.;METHODS: ;In vitro: Potency based on MIC90s was compared for 50 Staphylococcus aureus (SA), 50 Staphylococcus epidermidis (SE), and 25 each of Streptococcus pneumonia (SP), Streptococcus viridans (SV), Moraxella (MS), Haemophilus influenzae (HI), Pseudomonas aeruginosa (PA), and Serratia marcescens (SM). In vivo: Using established methods, ocular toxicity was graded with Draize testing. For efficacy testing, both corneas of 24 rabbits were infected with methicillin-resistant S. aureus (MRSA), whereas the corneal epithelium was removed in the left eye. After 4 h, 21 topical drops over 5 h were administered to 4 groups: BRI 0.5%, vancomycin (VAN) 5%, saline, and no treatment. The eyes were clinically graded and the corneas were harvested for colony counts.;RESULTS: ;In vitro: Both SA and SE had the lowest minimum inhibitory concentrations among the bacterial groups. The MIC90s to BRI for SP, SV, MS, HI, PA, and SM were 4, 32, 256, 32, 16, and 128-fold higher, respectively, than SA and SE. In vivo: Draize testing determined BRI 0.5% to be minimally irritating. For abraded corneas, BRI was not statistically different from VAN for reducing MRSA.

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