intrinsic

Bupranolol is an antagonist of β2-adrenergic receptor and has been used for angina pectoris, hypertension, glaucoma, cardiac arrhythmia and as an antithrombotic.

Beta-mangostin (β-Mangostin) is a xanthone compound with antibacterial and antimalarial activities. Beta-mangostin present in Cratoxylum arborescens and exhibits antimycobacterial activity against Mycobacterium tuberculosis with an MIC of 6.25 μg/mL. Beta-mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. Beta-mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic).

Bucindolol Formatel is a blocker of β1-adrenergic receptor. Bucindolol exhibits intrinsic sympathomimetic activity. Bucindolol can be used in the research of heart failure.

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.

ML353 (VU0478006) is a selective activator of TREK-1 and TREK-2 and a selective ligand (Ki =18.2 nM) for the mGlu5 Silencing Allosteric Modulator (SAM). ML353 has potential as a solution to the intrinsic activity or pharmacological blockade of SAM in vivo.

Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and no intrinsic sympathomimetic activity.

Carvedilol (SKF 105517) Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity. The S enantiomer of carvedilol nonselectively binds to and blocks beta-adrenergic receptors, thereby exerting negative inotropic and chronotropic effects, and leading to a reduction in cardiac output. In addition, both enantiomers of carvedilol bind to and block alpha 1-adrenergic receptors, thereby causing vasodilation and reducing peripheral vascular resistance.

Acebutolol hydrochloride (Acebutolol HCl) acts as a cardioselective beta-adrenergic antagonist with little effect on bronchial receptors and has intrinsic sympathomimetic properties. Acebutolol hydrochloride is the hydrochloride salt form of acebutolol, a synthetic butyranilide derivative with hypotensive and antiarrhythmic activity. Having stabilizing and quinidine-like effects on cardiac rhythm, Acebutolol hydrochloride is used in ventricular arrhythmias. Other indications include hypertension, alone or in combinations with other agents.

Cyanocobalamin is a cobalt-containing coordination compound generated by intestinal microbes and a natural water-soluble vitamin of the B-complex family that must combine with Intrinsic Factor for absorption by the intestine. Cyanocobalamin is necessary for hematopoiesis, neural metabolism, DNA, and RNA production, and carbohydrate, fat, and protein metabolism. B12 improves iron functions in the metabolic cycle and assists folic acid in choline synthesis. B12 metabolism is interconnected with that of folic acid. Vitamin B12 (Cobalamin) deficiency causes pernicious anemia, megaloblastic anemia, and neurologic lesions.

Carteolol hydrochloride (Abbott-43326) is a synthetic quinolinone derivative, antihypertensive Carteolol Hydrochloride is a nonselective beta-adrenoceptor blocking agent for beta-1 and beta-2 receptors with no membrane-stabilizing activity but moderate intrinsic sympathomimetic effects. It is used for the treatment of hypertension and certain arrhythmias and as an anti-angina and antiglaucoma agent.

Afurolol Hydrochloride (DL 071-IT) is a non-selective β-adrenergic receptor antagonist. DL 071 IT exhibits intrinsic sympathomimetic activity, reducing exercise heart rate, systolic blood pressure, and resting heart rate.

Bisoprolol, a selective beta-1 adrenergic receptor antagonist, selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, thereby with antihypertensive activity and devoid of intrinsic sympathomimetic activity.

Pindolol is an effective, non-selective, and specific beta-receptor blocker that acts as a partial beta-adrenergic receptor agonist and a localized 5-HT1A receptor antagonist (Ki=33nM). Pindolol has intrinsic sympathetic activity (ISA) and is primarily used to treat high blood pressure and certain heart conditions. Exhaustion.

Nivalenol is a fungal metabolite produced by Fusarium graminearum. Nivalenol induces cell death through caspase and intrinsic apoptotic pathways thus affecting the immune system and causing emesis, growth retardation, and reproductive disorders.

(±)15-HETE is an eicosanoid compound that possesses intrinsic biological activities and serves as a key enzymatic precursor for the biosynthesis of numerous other biologically active lipid-derived derivatives; furthermore, this alkyl chain-based structure functions as a proteolysis-targeting chimera (PROTAC) linker utilized in the chemical synthesis of various PROTAC molecules designed for targeted protein degradation.

LDN-214117 is a potent and selective ALK2 inhibitor.

Compound BPP (HDGFRP2/PSIP1-IN-1) is a dual inhibitor targeting the PWWP domains of Hepatoma-derived Growth Factor Related Protein 2 (HDGFRP2) and its homologue PSIP1. This compound effectively hinders the occurrence and progression of Diffuse Intrinsic Pontine Glioma (DIPG). It demonstrates binding affinity with a Kd value of 7 μM for HDGFRP2, indicative of its efficient ligand efficacy at 0.47. Additionally, Compound BPP exhibits a Kd value of 27 μM when binding to the PSIP1 PWWP domain, and a Kd value of 14 μM against HDGFRP3, confirming its potency as an inhibitor within the HDGFRP2 PWWP subfamily.

BCR-ABL-IN-10 (compound B4) is a covalent BCR-ABL inhibitor featuring an arylvinylsulfonate (AVS) moiety, demonstrating an IC50 of 43.1 nM against ABL kinase. It forms a covalent and stable adduct with ABL kinase, enabling the sustained inhibition of intrinsic BCR-ABL activity. This compound is utilized in the study of chronic myeloid leukemia (CML).

YM-31636 (free base) is an orally active, potent, and selective agonist of the 5-HT3 receptor with a pKi value of 9.67. This compound induces contraction in isolated guinea pig distal colon and provokes tachycardia in isolated guinea pig right atrium, demonstrating a relative intrinsic activity of about 0.23. YM-31636 (free base) holds potential for research in constipation management.

Ferrocene, a crucial structural core in bioorganometallic chemistry, is renowned for its intrinsic stability, excellent oxygen reduction capabilities, and low toxicity. It also exhibits antimalarial and anticancer properties.

M4K2308, a selective ALK2 ether-linked inhibitor, demonstrates an IC50 of 2 nM and exhibits greater specificity for ALK2 over ALK5, with an IC50 of 224 nM for ALK5. This compound holds potential for research into Diffuse Intrinsic Pontine Glioma (DIPG).

SUN90864, also known as 7-(2-Hydroxy-3-isopropylaminopropoxy)indene, is a potent β-adrenergic receptor blocker. It exhibits mild intrinsic β-sympathomimetic activity and local anesthetic effects. Additionally, SUN90864 is effective against arrhythmias induced by apomorphine and adrenaline.

INPYRFLUXAM, a benzamide fungicide, exhibits exceptionally high intrinsic activity. Studies indicate that for strains carrying SdhC-I88F, INPYRFLUXAM is the most potent SDHI fungicide, with an effective concentration (EC50) of just 0.0082 mg L-1.

EMT inhibitor-3 (compound 11i) is an epithelial-mesenchymal transition (EMT) inhibitor that effectively suppresses the proliferation, migration, and invasion of SK-N-SH neuroblastoma cells, with an IC50 value of 2.5 μM. It induces mitochondrial-mediated intrinsic apoptosis in tumor cells by enhancing the Bax/Bcl-2 protein expression ratio, promoting the release of cytochrome C from mitochondria, and activating caspase 9 and caspase 3. EMT inhibitor-3 is applicable for cancer research.