1224095-98-0|催乳素|Brilacidin|MFCD23726663-范德生物科技公司

催乳素

NMR下载 COA and HPLC MSDS下载
names：
Brilacidin
CAS号：
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)是一种抗菌剂，对革兰氏阳性菌肺炎链球菌和绿色链球菌的MIC90分别为1和8μg/ mL，对革兰氏阴性菌流感嗜血杆菌和铜绿假单胞菌的MIC90分别为8和4μg/ mL。溴酸是一种类似的防御素的抗生素（抗生素）。正在研究Brilacidin对粘膜炎，口腔炎，口腔疾病和头颈部肿瘤的支持治疗。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
YZM000175-1mg	1mg	>97%	¥ 9945.00	¥ 9945.00		2-3天	- +	¥ 0.00

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中文别名	催乳素(1224095-98-0);布雷西丁;PMX30063;布拉菌素; PMX30063；PMX-30063；PMX 30063；4-N，6-N-双[3- [5-（二氨基亚甲基亚氨基氨基）戊酰基氨基] -2-[（3R）-吡咯烷-3-基]氧基-5-（三氟甲基）苯基]嘧啶-4,6-二甲酰胺;
英文别名	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号	1224095-98-0
SMILES	O=C(C1=NC=NC(C(NC2=CC(C(F)(F)F)=CC(NC(CCCCNC(N)=N)=O)=C2O[C@H]3CNCC3)=O)=C1)NC4=CC(C(F)(F)F)=CC(NC(CCCCNC(N)=N)=O)=C4O[C@H]5CNCC5
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
闪点 FP
熔点 Melting point	No data available
沸点 Boiling point
Polarizability极化度	86.8±0.5 10-24cm3
密度 Density	1.6±0.1 g/cm3
蒸汽压 Vapor Pressure
溶解度Solubility
性状	固体粉末,Power
储藏条件 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)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染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:催乳素试剂催乳素杂质,催乳素合成,催乳素中间体,催乳素密度,催乳素溶解度,催乳素旋光度,催乳素闪点,催乳素熔点,催乳素购买,

产品说明	催乳素(Brilacidin,PMX 30063,1224095-98-0)是一种新型的防御素模拟物中的非肽类抗感染药,正在开发用于治疗眼部感染。
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)药理学：

一种对革兰氏阳性和革兰氏阴性细菌有效的研究性抗生素，这是一种以宿主防御肽（HDP）为模型的非肽小分子。目前正在治疗头颈部肿瘤以及粘膜炎的临床试验。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2413吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2393获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

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)参考文献：

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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