Brilacidin tetrahydrochloride

Name: Brilacidin tetrahydrochloride
SKU: GC60096
Availability: InStock
Rating: 5 (30 reviews)

(Synonyms: PMX 30063 tetrahydrochloride) 目录号 : GC60096

Brilacidin tetrahydrochloride (PMX-30063)是一种合成的、非肽的、小分子的宿主防御蛋白/肽(HDP)模拟物。

Brilacidin tetrahydrochloride Chemical Structure

Cas No.:1224095-99-1

规格价格库存购买数量

1mg	¥653.00	现货
5mg	¥1,350.00	现货
10mg	¥2,250.00	现货

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Sample solution is provided at 25 µL, 10mM.

GlpBio产品文献引用

Nature
610.7931 (2022): 366-372

Nature
618, 1017–1023 (2023)

Cell
183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

Cell Host Microbe
31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

产品文档

Quality Control & SDS

View current batch:

Purity: >98.50%

实验参考方法

Cell experiment [1]:
Cell lines	Calu-3 Cells
Preparation Method	Cells were placed in 96-well plates with 1.3×105 cells per well and allowed to adhere for 24 hours. Brilacidin tetrahydrochloride was dissolved in DMSO and then diluted in culture media to achieve the desired concentrations, ensuring that the final concentration of DMSO in the treatment did not exceed 0.1%. The cells were pre-treated with media containing the drug for 2 hours before infection. The virus was then allowed to incubate with the cells. After removing the virus, conditioned media containing the inhibitor were added to the cells.
Reaction Conditions	10-20 µM;2+24h
Applications	Brilacidin tetrahydrochloride inhibits SARS-CoV-2 in calu-3 cells.
Animal experiment [2]:
Animal models	C57BL/6 mice (fungal keratitis model)
Preparation Method	Each treatment involved applying 5 uL drops of the solution to the corneal surface of mice, done transiently for 5 minutes while the mice were under isoflurane anesthesia. Once the animals regained consciousness, their blink reflex and natural movement caused the drops to drain away. On day 0, the animals received a total of 3 treatments, starting at 4 hours apart and repeated every 3 hours thereafter. On day +1 and day +2, the animals received 6 treatments each, spaced 3 hours apart. Finally, on day +3, the animals received a single treatment.
Dosage form	5 uL,2.5 mM;16times in 3days
Applications	Brilacidin tetrahydrochloride blocks fungal growth and disease development in a murine model of fungal keratitis.
References: [1]. Bakovic A, Risner K, et,al. in Demonstrates Inhibition of SARS-CoV-2 in Cell Culture. Viruses. 2021 Feb 9;13(2):271. doi: 10.3390/v13020271. PMID: 33572467; PMCID: PMC7916214. [2]. Dos Reis TF, de Castro PA, et,al. A host defense peptide mimetic, brilacidin, potentiates caspofungin antifungal activity against human pathogenic fungi. Nat Commun. 2023 Apr 12;14(1):2052. doi: 10.1038/s41467-023-37573-y. PMID: 37045836; PMCID: PMC10090755.

产品描述

Brilacidin tetrahydrochloride (PMX-30063) is a synthetic, nonpeptidic, small-molecule mimetic of Host Defense Proteins/Peptides (HDPs). It exhibits broad-spectrum inhibitory activity in bacteria and viruses, and also has immunomodulatory capabilities and anti-inflammatory properties [1-3].

Brilacidin tetrahydrochloride, when used at concentrations of 10-20 µM for 24 hours, demonstrates strong ability to inhibit SARS-CoV-2 in a human lung cell line that expresses ACE2 (Calu-3 cells)^[4]. Brilacidin tetrahydrochloride (50µg/ ml;24h) inhibits replication-competent SARS-CoV-2 virus infection when added before viral entry^[5]. The combination of Brilacidin (40 µM; 24h) + ibrexafungerp is not toxic and reduces the A. fumigatus fungal burden during the infection of A549 lung epithelial cells[6].

Combining Brilacidin tetrahydrochloride with caspofungin (CAS) effectively eliminates A. fumigatus lung infection in an immunosuppressed murine model of invasive pulmonary aspergillosis. Additionally, Brilacidin tetrahydrochloride alone (administered at 5 uL, 2.5 mM concentration, repeated 16 times over 3 days) reduces A. fumigatus fungal load and prevents disease progression in a murine model of fungal keratitis^[6].

References:
[1]. Tew GN, Liu D, et,al. De novo design of biomimetic antimicrobial polymers. Proc Natl Acad Sci U S A. 2002 Apr 16;99(8):5110-4. doi: 10.1073/pnas.082046199. PMID: 11959961; PMCID: PMC122730.
[2]. Brilacidin as a Successful Example of de Novo Drug Design; Innovation Pharmaceuticals: Wakefield, MA, USA, 2017.
[3]. Mensa B, Howell GL, et,al. Comparative mechanistic studies of brilacidin, daptomycin, and the antimicrobial peptide LL16. Antimicrob Agents Chemother. 2014 Sep;58(9):5136-45. doi: 10.1128/AAC.02955-14. Epub 2014 Jun 16. PMID: 24936592; PMCID: PMC4135847.
[4]. Bakovic A, Risner K, et,al. Brilacidin Demonstrates Inhibition of SARS-CoV-2 in Cell Culture. Viruses. 2021 Feb 9;13(2):271. doi: 10.3390/v13020271. PMID: 33572467; PMCID: PMC7916214.
[5]. Xu C, Wang A, et,al. Brilacidin, a Non-Peptide Defensin-Mimetic Molecule, Inhibits SARS-CoV-2 Infection by Blocking Viral Entry. EC Microbiol. 2022 Apr;18(4):1-12. Epub 2022 Mar 8. PMID: 35695877; PMCID: PMC9186380.
[6]. Dos Reis TF, Diehl C, et,al. Brilacidin, a host defense peptide mimetic, potentiates ibrexafungerp antifungal activity against the human pathogenic fungus Aspergillus fumigatus. bioRxiv [Preprint]. 2024 Apr 5:2024.04.05.588305. doi: 10.1101/2024.04.05.588305. PMID: 38617338; PMCID: PMC11014541.
[7]. Dos Reis TF, de Castro PA, et,al. A host defense peptide mimetic, brilacidin, potentiates caspofungin antifungal activity against human pathogenic fungi. Nat Commun. 2023 Apr 12;14(1):2052. doi: 10.1038/s41467-023-37573-y. PMID: 37045836; PMCID: PMC10090755.

Brilacidin tetrahydrochloride (PMX-30063)是一种合成的、非肽的、小分子的宿主防御蛋白/肽(HDP)模拟物。它对细菌和病毒具有广谱抑制活性,并具有免疫调节能力和抗炎特性[1-3]。

Brilacidin tetrahydrochloride (10-20 µM;2+24h)在ACE2-positive的人肺细胞系(Calu-3细胞)中显示出对SARS-CoV-2的有效抑制[4]。在病毒进入前加入Brilacidin tetrahydrochloride (50µg/ ml;24h)可抑制复制能力强的SARS-CoV-2病毒感染[5]。Brilacidin tetrahydrochloride (40 µM; 24h) + ibrexafungerp联合使用无毒,可减少A549肺上皮细胞烟曲霉(A. fumigatus)感染[6]。

Brilacidin tetrahydrochloride联合卡泊芬净可明显清除侵袭性肺曲霉病免疫抑制小鼠模型中的烟曲霉肺感染。真菌性角膜炎小鼠模型中,单用Brilacidin tetrahydrochloride (5 uL,2.5 mM;16times in 3days)也可减少烟曲霉的真菌感染并减缓疾病发展[7]。

Chemical Properties

Cas No.	1224095-99-1	SDF
别名	PMX 30063 tetrahydrochloride
Canonical 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.Cl.Cl.Cl.Cl
分子式	C₄₀H₅₄Cl₄F₆N₁₄O₆	分子量	1082.75
溶解度	DMSO: 83.33 mg/mL (76.96 mM)	储存条件	Store at 2-8°C,sealed storage, away from moisture
General tips	请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。
Shipping Condition	评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。

溶解性数据

制备储备液
		1 mg	5 mg	10 mg
	1 mM	0.9236 mL	4.6179 mL	9.2357 mL
	5 mM	0.1847 mL	0.9236 mL	1.8471 mL
	10 mM	0.0924 mL	0.4618 mL	0.9236 mL

摩尔浓度计算器
稀释计算器
分子量计算器

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动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

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第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % saline

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计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系GLPBIO）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。