Delving into the Latest Updates on Tianjin Institute of Pharmaceutical Research Co., Ltd. with Synapse

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Other Diseases

Cardiovascular Diseases

Skin and Musculoskeletal Diseases

Small molecule drug

Herbal medicine

Fusion protein

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Endocrinology and Metabolic Disease	3
Nervous System Diseases	2
Infectious Diseases	2
Immune System Diseases	2
Neoplasms	1

Top 5 Drug Type	Count

Small molecule drug	14
Herbal medicine	5
Fusion protein	1

Top 5 Target	Count

CaM x Nav1.5	1
SGLT2(Sodium/glucose cotransporter 2)	1
factor Xa	1
5-LOX x COX-2	1
DRDs(Dopamine receptors)	1

主要目的： 1.评价泰普格雷片在中国健康受试者中的药代动力学（PK）特征和药效学（PD）特征； 2.比较泰普格雷与氯吡格雷的药代动力学和药效学特征； 3.比较泰普格雷与替格瑞洛的药效学特征。次要目的：评价泰普格雷片在中国健康受试者中的安全性。

[Translation]

Main objectives: 1. To evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) characteristics of Tapogrel tablets in healthy Chinese subjects; 2. To compare the pharmacokinetic and pharmacodynamic characteristics of Tapogrel and clopidogrel; 3. To compare the pharmacodynamic characteristics of Tapogrel and ticagrelor. Secondary objectives: To evaluate the safety of Tapogrel tablets in healthy Chinese subjects.

Start Date09 Sep 2024

Sponsor / Collaborator

Tianjin Institute of Pharmaceutical Research Co., Ltd.

100 Clinical Results associated with Tianjin Institute of Pharmaceutical Research Co., Ltd.

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0 Patents (Medical) associated with Tianjin Institute of Pharmaceutical Research Co., Ltd.

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762

Literatures (Medical) associated with Tianjin Institute of Pharmaceutical Research Co., Ltd.

01 Oct 2024·Neurochemical Research

Neuroprotection of Human Umbilical Cord-Derived Mesenchymal Stem Cells (hUC-MSCs) in Alleviating Ischemic Stroke-Induced Brain Injury by Regulating Inflammation and Oxidative Stress

Article

Author: Liu, Guangyang ; Xu, Xiaodan ; Liu, Yongjun ; Zhou, Jingwen ; Xu, Liqiang ; Miao, Li ; Jia, Jianru ; Chen, Yaoyao ; Mi, Yi ; Wang, Daohui ; Ge, Qinggang ; Li, Xin ; Zhang, Chenliang ; Wang, Herui ; Hao, Chunhua

Brain injury caused by stroke has a high rate of mortality and remains a major medical challenge worldwide. In recent years, there has been significant attention given to the use of human Umbilical cord-derived Mesenchymal Stem Cells (hUC-MSCs) for the treatment of stroke in different adult and neonate animal models of stroke. However, using hUC-MSCs by systemic administration to treat ischemic stroke has not been investigated sufficiently. In this study, we conducted various experiments to explore the neuroprotection of hUC-MSCs in rats. Our findings demonstrate that an intravenous injection of a high dose of hUC-MSCs at 2 × 10^7 cells/kg markedly ameliorated brain injury resulting from ischemic stroke. This improvement was observed one day after inducing transient middle cerebral artery occlusion (MCAO) and subsequent reperfusion in rats. Notably, the efficacy of this single administration of hUC-MSCs surpassed that of edaravone, even when the latter was used continuously over three days. Mechanistically, secretory factors derived from hUC-MSCs, such as HGF, BDNF, and TNFR1, ameliorated the levels of MDA and T-SOD to regulate oxidative stress. In particular, TNFR1 also improved the expression of NQO-1 and HO-1, important proteins associated with oxidative stress. More importantly, TNFR1 played a significant role in reducing inflammation by modulating IL-6 levels in the blood. Furthermore, TNFR1 was observed to influence the permeability of the blood-brain barrier (BBB) as demonstrated in the evan's blue experiment and protein expression of ZO-1. This study represented a breakthrough in traditional methods and provided a novel strategy for clinical medication and trials.

01 Sep 2024·Journal of Pharmaceutical Analysis

Automated and integrated ultrahigh throughput screening for industrial strain enabled by acoustic-droplet-ejection mass spectrometry

Article

Author: Han, Zhibo ; Zhong, Shasha ; Zheng, Ping ; Zhang, Zhidan ; Sun, Jibin ; Cai, Ningyun ; Zhang, Chao ; Zhu, Yan ; Chen, Jiuzhou ; Liu, Changxiao ; Zhang, Xu

Image 1.

01 Aug 2024·Journal of Ethnopharmacology

Ligustilide covalently binds to Cys703 in the pre-S1 helix of TRPA1, blocking the opening of channel and relieving pain in rats with acute soft tissue injury

Article

Author: Jiang, Min ; Hou, Yuanyuan ; Zhang, Kaixue ; Fu, Cheng ; Liu, Wenjuan ; Wu, Weidong ; Shen, Fukui ; Han, Yanqi ; Luan, Guoqing ; Xu, Jun ; Bai, Gang ; Zhang, Tiejun

ETHNOPHARMACOLOGICAL RELEVANCEThe natural anodyne Ligustilide (Lig), derived from Angelica sinensis (Oliv.) Diels and Ligusticum chuanxiong Hort., has been traditionally employed for its analgesic properties in the treatment of dysmenorrhea and migraine, and rheumatoid arthritis pain. Despite the existing reports on the correlation between TRP channels and the analgesic effects of Lig, a comprehensive understanding of their underlying mechanisms of action remains elusive.AIM OF THE STUDYThe objective of this study is to elucidate the mechanism of action of Lig on the analgesic target TRPA1 channel.METHODSThe therapeutic effect of Lig was evaluated in a rat acute soft tissue injury model. The analgesic target was identified through competitive inhibition of TRP channel agonists at the animal level, followed by Fluo-4/Ca²⁺ imaging on live cells overexpressing TRP proteins. The potential target was verified through in-gel imaging, colocalization using a Lig-derived molecular probe, and a drug affinity response target stability assay. The binding site of Lig was identified through protein spectrometry and further analyzed using molecular docking, site-specific mutation, and multidisciplinary approaches.RESULTSThe administration of Lig effectively ameliorated pain and attenuated oxidative stress and inflammatory responses in rats with soft tissue injuries. Moreover, the analgesic effects of Lig were specifically attributed to TRPA1. Mechanistic studies have revealed that Lig directly activates TRPA1 by interacting with the linker domain in the pre-S1 region of TRPA1. Through metabolic transformation, 6,7-epoxyligustilide (EM-Lig) forms a covalent bond with Cys703 of TRPA1 at high concentrations and prolonged exposure time. This irreversible binding prevents endogenous electrophilic products from entering the cysteine active center of ligand-binding pocket of TRPA1, thereby inhibiting Ca²⁺ influx through the channel opening and ultimately relieving pain.CONCLUSIONSLig selectively modulates the TRPA1 channel in a bimodal manner via non-electrophilic/electrophilic metabolic conversion. The epoxidized metabolic intermediate EM-Lig exerts analgesic effects by irreversibly inhibiting the activation of TRPA1 on sensory neurons. These findings not only highlight the analgesic mechanism of Lig but also offer a novel nucleophilic attack site for the development of TRPA1 antagonists in the pre-S1 region.

100 Deals associated with Tianjin Institute of Pharmaceutical Research Co., Ltd.

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100 Translational Medicine associated with Tianjin Institute of Pharmaceutical Research Co., Ltd.

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Pipeline

Pipeline Snapshot as of 26 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Discovery

1

3

Preclinical

IND Approval

2

4

Phase 1 Clinical

Phase 2 Clinical

8

2

Phase 3 Clinical

Approved

2

11

Other

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Aprindine Hydrochloride ( CaM x Nav1.5 )	Arrhythmias, Cardiac More	Approved
Pipotiazine Palmitate ( DRDs )	Schizophrenia More	Approved
Compound Caraway Enteric Liquid Capsule	Dyspepsia More	Phase 3
TY1801J	Onychomycosis More	Phase 3
Tianagliflozin ( SGLT2 )	Diabetes Mellitus, Type 2 More	Phase 2