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SQ109

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squalene synthase Inhibitor
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基本描述

规格或纯度 ≥99%
英文名称 SQ109
英文别名 NSC 722041；SQ-109； N'-(2-adamantyl)-N-[(2E)-3,7-dimethylocta-2,6-dienyl]ethane-1,2-diamine
生化机理

SQ109 is an orally active, small molecule antibiotic for treatment of pulmonary T(tuberculosis). In Phase I clinical trials, SQ109 could replace one or more drμgs in the current first-line TB drμg regimen, simplify therapy, and shorten the TB treatment regimen. SQ109 has excellent in vitro activity against Mycobacterium tuberculosis within a MIC range of 1-0.5 μM (drμg susceptible) and drμg resistant TB bacteria, including XDR-TB, as well as potent in vivo activity against pulmonary TB alone and with other TB drμgs.

储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

产品介绍：

SQ109是一种抗生素小分子。

名称和标识符

IUPAC Name N'-(2-adamantyl)-N-[(2E)-3,7-dimethylocta-2,6-dienyl]ethane-1,2-diamine
INCHI InChI=1S/C22H38N2/c1-16(2)5-4-6-17(3)7-8-23-9-10-24-22-20-12-18-11-19(14-20)15-21(22)13-18/h5,7,18-24H,4,6,8-15H2,1-3H3/b17-7+
InChi Key JFIBVDBTCDTBRH-REZTVBANSA-N
Canonical SMILES CC(=CCCC(=CCNCCNC1C2CC3CC(C2)CC1C3)C)C
分子式

C22H38N2
PubChem CID 5274428
分子量 330.55

化学和物理性质

溶解性 DMSO

靶标

Target ID 645
名称 squalene synthase
缩写名 SHP2
家族 Lanosterol biosynthesis pathway
别名 IL-8R1
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 2 417 8p23.1 FDFT1 farnesyl-diphosphate farnesyltransferase 1
Mouse 2 416 14 33.24 cM Fdft1 farnesyl diphosphate farnesyl transferase 1
Rat 2 416 15p12 Fdft1 farnesyl diphosphate farnesyl transferase 1
Entrez Gene 2222 (Hs) , 14137 (Mm) , 29580 (Rn)
OMIM 184420 (Hs)
UniProtKB P37268 (Hs) , P53798 (Mm) , Q02769 (Rn)
Ensembl Gene ENSG00000079459 (Hs) , ENSRNOG00000021314 (Rn) , ENSMUSG00000021273 (Mm)
RefSeq Nucleotide NM_004462 (Hs) , NM_010191 (Mm) , NM_019238 (Rn)
RefSeq Protein NP_004453 (Hs) , NP_034321 (Mm) , NP_114028 (Rn)
Protein GI 67089147 (Hs) , 34328173 (Mm) , 9506591 (Rn)
CATH/Gene3D 1.10.600.10 (N/A)
ChEMBL Target CHEMBL3815 (Rn) , CHEMBL4778 (Mm) , CHEMBL3338 (Hs)

关联配体

Ligand ID 7997
名称 SQ-109
别名 SQ 109
类别 Synthetic organic
学名 N'-(2-adamantyl)-N-[(2E)-3,7-dimethylocta-2,6-dienyl]ethane-1,2-diamine
生物活性评价 SQ-109 has activity against both drug susceptible and multidrug resistant strains of M. tuberculosis (MIC of 0.7-1.56 μM in vitro) .
评价 SQ-109 is a [1,2]-diamine-based ethambutol analogue included in the Medicines for Malaria Pandemic Response Box (MMV PRB). Functionally, it inhibits Mycobacterial membrane protein large 3 (MmpL3) and has advanced to clinical evaluation for the treatment of tuberculosis .

The compound also has antimalarial activity. The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
配体家族 Antimalarial ligands
临床描述 This study is a multiple-arm, multiple-stage (MAMS), phase 2, open label, randomized, controlled clinical trial that will compare the efficacy and safety of four experimental four drug regimens with a standard control regimen in patients with smear positive, pulmonary tuberculosis (TB). Patients will be randomly allocated to the control or one of the four experimental regimens in the ratio 2:1:1:1:1. Experimental regimens will be given for 12 weeks. Thereafter, participants in the experimental arms will receive continuation phase treatment for 14 weeks containing standard-dose rifampicin and isoniazid. All participants will receive 25 mg of vitamin B6 (pyridoxine) with every dose of INH to prevent INH-related neuropathy. Interim analyses will be conducted during the trial for efficacy, with the aim of identifying experimental arms that perform below a pre-specified efficacy threshold; these arms will then be stopped from further recruitment. Following the first scheduled interim analysis on March 3rd, the Trial Steering Committee (TSC) followed a recommendation of the independent data monitoring committee (IDMC) and has stopped the enrolment into two of the arms in the MAMS-TB trial: HRZQ and HR20ZQ, based on these arms not meeting the pre-specified gain in efficacy over control. Importantly, there was no safety concern that prompted stopping recruitment to these arms. They recommended that recruitment to arm 2 (HRZQ) and 3 (HR20ZQ) be terminated as there was insufficient evidence that these regimens could shorten treatment. Importantly, there was no evidence that either arm was inferior to standard treatment (the control arm) with regards to efficacy. There was, however, sufficient evidence that the other intervention arms HR35ZE and HR20ZM could shorten treatment to continue enrolling patients.
SQ109 was developed with the aim of shortening TB treatment and providing new drugs for resistant TB. The drug has demonstrated efficacy in toxicology studies and an acceptable safety profile in first-in-man studies. The objective of this study is to evaluate the extended early bactericidal activity (EBA), safety, tolerability, and pharmacokinetics of several doses of SQ109 with or without Rifampicin (RIF) for 14 days in adults with newly diagnosed, uncomplicated, smear positive, pulmonary TB.
来源公司 Ludwig-Maximilians - University of Munich
Ludwig-Maximilians - University of Munich

参考文献

1. Protopopova M, Hanrahan C, Nikonenko B, Samala R, Chen P, Gearhart J, Einck L, Nacy CA.  (2005)  Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines..  J Antimicrob Chemother,  56  (5):  (968-74).  [PMID:16172107]
2. Tahlan K, Wilson R, Kastrinsky DB, Arora K, Nair V, Fischer E, Barnes SW, Walker JR, Alland D, Barry 3rd CE et al..  (2012)  SQ109 targets MmpL3, a membrane transporter of trehalose monomycolate involved in mycolic acid donation to the cell wall core of Mycobacterium tuberculosis..  Antimicrob Agents Chemother,  56  (4):  (1797-809).  [PMID:22252828]
3. Boeree MJ, Heinrich N, Aarnoutse R, Diacon AH, Dawson R, Rehal S, Kibiki GS, Churchyard G, Sanne I, Ntinginya NE et al..  (2017)  High-dose rifampicin, moxifloxacin, and SQ109 for treating tuberculosis: a multi-arm, multi-stage randomised controlled trial..  Lancet Infect Dis,  17  (1):  (39-49).  [PMID:28100438]
4. Reader J, van der Watt ME, Taylor D, Le Manach C, Mittal N, Ottilie S, Theron A, Moyo P, Erlank E, Nardini L et al..  (2021)  Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box..  Nat Commun,  12  (1):  (269).  [PMID:33431834]
5. Zhang B, Li J, Yang X, Wu L, Zhang J, Yang Y, Zhao Y, Zhang L, Yang X, Yang X et al..  (2019)  Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target..  Cell,  176  (3):  (636-648.e13).  [PMID:30682372]

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